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The formation of a core–shell structure by coating silicon (Si) nanoparticles with a carbon layer is considered a promising method to address the poor conductivity of a Si-based anode and volume expansion of silicon particles during the charging/discharging process. However, Si/C composite anodes usually perform below expectations with a single layer of carbon utilized as the coating layer, while introducing multilayer carbon coating results in the additional complexity and cost. To overcome this challenge, in this work, waterborne polyurethane (WPU) had been simply mixed with the Si nanoparticles to form the Si/WPU composite via the hydrogen bonds, and the core–shell structure with the single carbon layer containing N atoms (Si@NC) was obtained after the pyrolysis of the composite. The carbon layer not only significantly alleviated the breakage of the anode caused by the volume expansion of Si nanoparticles but also optimized the rate performance of the anode. At a current density of 0.5 A g–1, the discharge specific capacity of the Si@NC anode is still as high as 945.63 mAh g–1 after 300 cycles, surpassing various single-layer carbon and multilayer carbon-coated Si-based anodes. This work provides a convenient and feasible method for preparing economical Si/C composite anode materials. [ABSTRACT FROM AUTHOR]

Assembling transition-metal oxides (TMOs) and MXene with strong interfacial interactions is an effective method to overcome the drawbacks of TMOs as anodes for lithium-ion batteries (LIBs) such as large volume expansion and low conductivity. Herein, a CuO nanorod/MXene heterojunction (denoted as CuO/MXene) with a synergistic effect was constructed with a "sheet-rod-pore" hierarchical nanostructure by electrostatic self-assembly. Specifically, encapsulated CuO nanorods exert superiority in the high reversible capacity and increase the interlayer distance of the MXene matrix to explore more storage spaces. MXene could significantly boost the conductivity, accommodate volume variation, and inhibit structure collapse as a buffer network. Density functional theory (DFT) calculations confirm the strong electron transport and lithium affinity at the CuO/MXene heterointerface, elucidating the reasons for the enhanced lithium storage capacity (436.4 mAh g–1 at 500 mA g–1), ion diffusion kinetics, and structural stability after cycling than pure CuO and MXene. When paired with the LiCoO2 cathode, the full cell delivers good cycling stability after 140 cycles, indicating the practical applicability of CuO/MXene. This work not only validates the robust interfacial interaction of TMO/MXene heterojunction but also explores an effective strategy to prepare promising anode materials for the next-generation LIBs. [ABSTRACT FROM AUTHOR]

A series of ternary Cu-ZnO-ZrO2 nanostructures was prepared containing either tetrapropylammonium hydroxide (TPAOH, TH), polyoxyethylene lauryl ether carboxylic acid (BRIJ35, B5), poly-(ethylene oxide)-poly-(propylene oxide)-poly-(ethylene oxide) (P123 P3), decyltrimethylammonium bromide (DB), poly-(vinylpyrrolidone) (PVP, PP), or no surfactant. First, based on the characterization results of XPS, H2-TPR, and other characteristics, the Cu species play vital roles in the process of dimethyl adipate (DMA) hydrogenation, and the Cu+ and Cu0 generated after reduction have a synergistic effect in the hydrogenation process. Results showed that changing the surfactant type and surfactant concentration in the catalyst synthesis has a great effect on the catalytic activity of the catalyst. In particular, the HDO selectivity of the CZZ-4-P3 (52%) catalyst treated with poly-(ethylene oxide)-poly-(propylene oxide)-poly-(ethylene oxide) was significantly improved compared to the untreated CZZ (29%) catalyst, which is related to the highest concentration and number of oxygen vacancies. The larger amount of Ovac might promote the hydrogenation of DMA through interaction with the carbonyl group and then weaken the CO bond. On the other hand, it also has a more surface basic (strong basic) amount on the CZZ catalyst. This will provide more adsorption sites and thus adsorb more DMA molecule. Furthermore, it has a larger dispersion of the Cu and smaller catalyst particles. This may be more conducive to adequate contact between the feedstock and catalyst, reducing diffusion effects. [ABSTRACT FROM AUTHOR]

Matrix isolated infrared spectroscopic and density functional theoretical calculations of the GeO2 - and GeO4 (super -) anions are examined. The GeO2 (super -) anion is concluded to be bent with a bond angle.

Zeolite nanocrystals are used as building blocks to fabricate complex porous structures, such as micropatterned zeolite films.

Stearicand oleic acid-coated Fe3O4nanoparticles weredispersed in decahydronaphthalene (DN). This oil phase was dispersedin water using ternary graft copolymer poly(glycidyl methacrylate)-graft-[polystyrene-ran-(methoxy polyethyleneglycol)-ran-poly(2-cinnamoyloxyethyl methacrylate)]or PGMA-g-(PS-r-MPEG-r-PCEMA) to yield capsules. The walls of these capsules were composedof PCEMA chains that were soluble in neither water nor DN, and theDN-soluble PS chains stretched into the droplet phase and the water-solubleMPEG chains extended into the aqueous phase. Structurally stable capsuleswere prepared by photolyzing the capsules with UV light to cross-linkthe PCEMA layer. Both the magnetite particles and the magnetite-containingcapsules were superparamagnetic. The sizes of the capsules increasedas they were loaded with more magnetite nanoparticles, reaching amaximal loading of ∼0.5 mg of ligated magnetite nanoparticlesper mg of copolymer. But the radii of the capsules were always <100nm. Thus, a novel nanomaterialsuperparamagnetic-oil-filledpolymer nanocapsuleswas prepared. The more heavily loadedcapsules were readily captured by a magnet and could be redispersedvia shaking. Although the cross-linked capsules survived this capturingand redispersing treatment many times, the un-cross-linked capsulesruptured after four cycles. These results suggest the potential totailor-make capsules with tunable wall stability for magneticallycontrolled release applications. [ABSTRACT FROM AUTHOR]

Degradability is vital for bone filling and plays an important role in bone regeneration. Evidence indicates that apatite-based calcium phosphate cement (ACPC) is a prospective biomaterial for bone repair with enhanced osteogenesis. However, poor degradability restricts their clinical application. In this study, MgZnCa-doped ACPC (MgZnCa/ACPC) composites were fabricated by adding 3 (wt) % amorphous MgZnCa powder in the solid phase of ACPC to enhance the biodegradation and bioactivity of the apatite ACPC. The chemical and the physical properties of the MgZnCa/ACPC composite were investigated and compared with the ACPC composite. The results showed that the incorporation of MgZnCa improved both the degradability and the compressive strength of the ACPC composite. X-ray diffraction and Fourier transform infrared spectrometry analysis suggested significant changes in the microstructures of the composites due to the incorporation and the anodic dissolution of MgZnCa alloy. These findings indicate that the MgZnCa/ACPC composite is capable of facilitating bone repair and regeneration by endowing favorable degradation property.

KNbO 3 (KN) with a perovskite structure is an outstanding representative of lead-free piezoelectric materials, and its mesocrystals have broad application prospects in the fields of catalysis, energy storage, and conversion. However, the formation conditions of KN mesocrystals reported so far are difficult owing to their high aspect ratio and excellent preferred orientation. In this study, the solvothermal process was used successfully to prepare the flake-like potassium salt of Lindquist hexaniobate (K 8 Nb 6 O 19 ·10H 2 O). Subsequently, the precursor niobate was calcined to prepare two-dimensional (2D) plate-like KN mesocrystals. The formation mechanism of the plate-like KN mesocrystals is further revealed from a paired topochemical mesocrystal conversion of K 8 Nb 6 O 19 ·10H 2 O niobate. Finally, the microscopic piezoelectric and photocatalytic responses of the obtained plate-like KN mesocrystals were investigated. The high piezoelectric coefficient of plate-like KN mesocrystals implies that excellent charge separation promotes the photocatalytic performance of rhodamine B (RhB). This study provides a strategy for the efficient application of 2D oriented materials in the field of piezoelectricity and photocatalysis.

A wearable thermoelectric cooler (w-TEC) shows promising prospects in personal thermal management due to its zero emission, high efficiency, lightweight, and long-term stability. The flexible heatsinks are able to promote the cooling effect of coolers, but the cooling capacity of current coolers still has much room for improvement because of the relatively large thermal resistance between the cooler and heatsink. In this work, the two-layer heatsink units composed of hydrogel and nickel foam are fabricated and attached to a thermoelectric cooler via the thermal silica gel. Thanks to the high thermal conductivity of nickel foam and a tight bond between the hydrogel and nickel foam, effective heat conduction from the cooler to the body of the heatsink was achieved. In addition, the discrete heatsink units endow the w-TEC with excellent flexibility. The bending radius of this w-TEC is as small as 7.5 mm, and a long-term temperature reduction of ∼10 °C can be realized at an input current of 0.3 A for a flat or bent w-TEC. In the on-body testing, a stable temperature reduction of 7 °C can be obtained using an AA battery with an input voltage of 1.5 V.

Wearable thermoelectric generators (w-TEGs) can incessantly convert body heat into electricity to power electronics. However, the low efficiency of thermoelectric materials, tiny terminal temperature difference, rigidity, and negligence of lateral heat transfer preclude broad utilization of w-TEGs. In this work, we employ finite element simulation to find the key factors for simultaneous realization of flexibility and ultrahigh normalized power density. Using melamine foam with an ultralow thermal conductivity (0.03 W/m K) as the encapsulation material, a novel lightweight π-type w-TEG with no heatsink and excellent stretchability, comfortability, processability, and cost efficiency has been fabricated. At an ambient temperature of 24 °C, the maximum power density of the w-TEG reached 7 μW/cm 2 (sitting) and 29 μW/cm 2 (walking). Under suitable heat exchange conditions (heatsink with 1 m/s air velocity), 32 pairs of w-TEGs can generate 66 mV voltage and 60 μW/cm 2 power density. The output performance of our TEG is remarkably superior to that of previously reported w-TEGs. Besides, the practicality of our w-TEG was showcased by successfully driving a quartz watch at room temperature.

Half-Heusler alloys, which possess the advantages of high thermal stability, a large power factor, and good mechanical property, have been attracting increasing interest in mid-temperature thermoelectric applications. In this work, extra Zr-doped TiZr x NiSn samples were successfully prepared by a modified solid-state reaction followed by spark plasma sintering. It demonstrates that extra Zr doping could not only improve the power factor on account of an increase in the Seebeck coefficient but also suppress the lattice thermal conductivity originated from the strengthened phonon scattering by the superlattice nanodomains and the secondary nanoparticles. As a consequence, an increased power factor of 3.29 mW m -1 K -2 and a decreased lattice thermal conductivity of 1.74 W m -1 K -1 are achieved in TiZr 0.015 NiSn, leading to a peak ZT as high as 0.88 at 773 K and an average ZT value up to 0.62 in the temperature range of 373-773 K. This work gives guidance for optimizing the thermoelectric performance of TiNiSn-based alloys by modulating the microstructures on the secondary nanophases and superlattice nanodomains.

Mg 3 Sb 2 -based compounds by virtue of nontoxicity and low-cost have become a promising class of candidates for midtemperature thermoelectric power generation. Here, we successfully fabricated n-type Mg 3 Sb 2 -based materials using an inexpensive and efficient approach of one-step ball milling and spark plasma sintering, and demonstrate that a complementary and favorable effect of multiple elements coalloying/-doping leads to an excellent thermoelectric performance. The intrinsic p-type conducting behavior for Mg 3 Sb 2 could be changed to n-type through Bi and Se coalloying on Sb sublattices with excess Mg, resulting from the suppression of Mg vacancies and the formation of Mg interstitial. Furthermore, Mn doping on Mg sublattices could soften the chemical bonds, leading to the increase of carrier mobility and concentration simultaneously. Additionally, multielement coalloying/-doping could significantly increase the lattice disorder, which undoubtedly strengthens the phonon scattering and readily results in a suppressed lattice thermal conductivity. As a result, a highest ZT value of 1.6 at 723 K and an average ZT value up to 1.1 were obtained in the temperature range of 323-723 K in the Mg 3.18 Mn 0.02 Sb 1.5 Bi 0.49 Se 0.01 sample, which is one of the highest values among the Te free Mg 3 Sb 2 . This work could give guidance for improving the thermoelectric performance of Zintl phase materials or even others using the multielement codoping/-alloying strategy.

Anti-apoptotic Bcl-2 family proteins are overexpressed in a wide spectrum of cancers and have become well validated therapeutic targets. Cancer cells display survival dependence on individual or subsets of anti-apoptotic proteins that could be effectively targeted by multimodal inhibitors. We designed a 2,5-substituted benzoic acid scaffold that displayed equipotent binding to Mcl-1 and Bfl-1. Structure-based design was guided by several solved cocrystal structures with Mcl-1, leading to the development of compound 24 , which binds both Mcl-1 and Bfl-1 with K i values of 100 nM and shows appreciable selectivity over Bcl-2/Bcl-xL. The selective binding profile of 24 was translated to on-target cellular activity in model lymphoma cell lines. These studies lay a foundation for developing more advanced dual Mcl-1/Bfl-1 inhibitors that have potential to provide greater single agent efficacy and broader coverage to combat resistance in several types of cancer than selective Mcl-1 inhibitors alone.

At present, copper sulfide materials have been predicted as promising thermoelectric materials due to their inexpensiveness and nontoxicity property. Most researches on copper sulfide are focused on Cu 2 S and Cu 1.8 S because they are more easily synthesized into a single phase; however, the improper electrical conductivity greatly hindered their thermoelectric properties. In this work, a series of high-performance Cu 1.9- x Ni x S ( x = 0, 0.01, 0.015, and 0.02) bulk samples were fabricated by accurately manipulating the ratio of Cu/S with appropriate Ni-doping. The thermoelectric properties of Ni-doped Cu 1.9 S were explored in detail for the first time. It can be found that carrier thermal conductivity and lattice thermal conductivity of Cu 1.9- x Ni x S were effectively reduced via Ni-doping, simultaneously, without the great influence on the power factor. Here, the carrier thermal conductivity (κ e ) was reduced due to the extreme reduction of Hall carrier concentration. In addition, amounts of nanopores introduced by Ni-doping and complex crystal structure from the phase transition of the second phase strengthen the phonon scattering and reduce lattice thermal conductivity (κ l ) remarkably. As a consequence, the lowest carrier thermal conductivity and lattice thermal conductivity reach 0.006 and 1.08 W m -1 K -1 for Cu 1.88 Ni 0.02 S at 773 K, and the average ZT is about 0.39 from 323 to 773 K (the ZT max is about 0.9 at 773 K). This work demonstrates that low-cost and easily fabricated Ni-doped Cu 1.9 S is a pleasurable candidate for thermoelectric application despite it usually being treated as an ion conductor.

Pancreatic tumors are known to be resistant to immunotherapy due to the extensive immune suppressive tumor microenvironment (TME). We hypothesized that CXCL12 and PD-L1 are two key molecules controlling the immunosuppressive TME. Fusion proteins, called traps, designed to bind with these two molecules with high affinity (K d = 4.1 and 0.22 nM, respectively) were manufactured and tested for specific binding with the targets. Plasmid DNA encoding for each trap was formulated in nanoparticles and intravenously injected to mice bearing orthotopic pancreatic cancer. Expression of traps was mainly seen in the tumor, and secondarily, accumulations were primarily in the liver. Combination trap therapy shrunk the tumor and significantly prolonged the host survival. Either trap alone only brought in a partial therapeutic effect. We also found that CXCL12 trap allowed T-cell penetration into the tumor, and PD-L1 trap allowed the infiltrated T-cells to kill the tumor cells. Combo trap therapy also significantly reduced metastasis of the tumor cells to other organs. We conclude that the trap therapy significantly modified the immunosuppressive TME to allow the host immune system to kill the tumor cells. This can be an effective therapy in clinical settings.

Our previous work demonstrated that Wnt16 expression in cisplatin-damaged tumor-associated fibroblasts is a key factor contributing to cisplatin resistance in malignancies. Natural antifibrotic compounds with low toxicities are promising candidates to downregulate Wnt16 expression, improving the antitumor effect of cisplatin nanoparticles. Upon screening several natural chemicals, we found that a dietary flavonoid, quercetin, significantly suppresses Wnt16 expression in activated fibroblasts. To facilitate drug delivery, we have prepared a targeted lipid/calcium/phosphate nanoparticle formulation consisting of a prodrug of quercetin, i.e., quercetin phosphate, with a high loading efficiency (26.6% w/w). This quercetin nanoparticle with a particle size of around 35 nm significantly improved the bioavailability and metabolic stability of the parent quercetin. Quercetin phosphate is released from the nanoparticles and converted back to the parent quercetin under physiological conditions. Following systemic administration of quercetin phosphate nanoparticles, a significant downregulation in Wnt16 expression was observed and further yielded a synergistic antitumor effect with cisplatin nanoparticles in a stroma-rich bladder carcinoma model. The α-SMA-positive fibroblast and collagen within the tumor decreased significantly after combination treatment. This suggests that the remodeling of the tumor microenvironment induced by quercetin plays a critical role in promoting the synergy. Indeed, our data further confirmed that quercetin phosphate alone significantly remodeled the tumor microenvironment and increased the penetration of second-wave nanoparticles into the tumor nests. Collectively, quercetin phosphate nanoparticles may be a safe and effective way to improve therapeutic treatment for desmoplastic tumors.

The binding site barrier (BSB) was originally proposed to describe the binding behavior of antibodies to cells peripheral to blood vessels, preventing their further penetration into the tumors. Yet, it is revisited herein to describe the intratumoral cellular disposition of nanoparticles (NPs). Specifically, the BSB limits NP diffusion and results in unintended internalization of NPs by stroma cells localized near blood vessels. This not only limits the therapeutic outcome but also promotes adverse off-target effects. In the current study, it was shown that tumor-associated fibroblast cells (TAFs) are the major component of the BSB, particularly in tumors with a stroma-vessel architecture where the location of TAFs aligns with blood vessels. Specifically, TAF distance to blood vessels, expression of receptor proteins, and binding affinity affect the intensity of the BSB. The physical barrier elicited by extracellular matrix also prolongs the retention of NPs in the stroma, potentially contributing to the BSB. The influence of particle size on the BSB was also investigated. The strongest BSB effect was found with small (∼18 nm) NPs targeted with the anisamide ligand. The uptake of these NPs by TAFs was about 7-fold higher than that of the other cells 16 h post-intravenous injection. This was because TAFs also expressed the sigma receptor under the influence of TGF-β secreted by the tumor cells. Overall, the current study underscores the importance of BSBs in the delivery of nanotherapeutics and provides a rationale for exploiting BSBs to target TAFs.

Chemotherapeutic efficacy can be greatly improved by developing nanoparticulate drug delivery systems (nano-DDS) with high drug loading capacity and smart stimulus-triggered drug release in tumor cells. Herein, we report a novel redox dual-responsive prodrug-nanosystem self-assembled by hydrophobic small-molecule conjugates of paclitaxel (PTX) and oleic acid (OA). Thioether linked conjugates (PTX-S-OA) and dithioether inserted conjugates (PTX-2S-OA) are designed to respond to the redox-heterogeneity in tumor. Dithioether has been reported to show redox dual-responsiveness, but we find that PTX-S-OA exhibits superior redox sensitivity over PTX-2S-OA, achieving more rapid and selective release of free PTX from the prodrug nanoassemblies triggered by redox stimuli. PEGylated PTX-S-OA nanoassemblies, with impressively high drug loading (57.4%), exhibit potent antitumor activity in a human epidermoid carcinoma xenograft. This novel prodrug-nanosystem addresses concerns related to the low drug loading and inefficient drug release from hydrophobic prodrugs of PTX, and provides possibilities for the development of redox dual-sensitive conjugates or polymers for efficient anticancer drug delivery.

Antimony telluride (Sb2Te3) and its based alloys are of importance to p-type semiconductors for thermoelectric applications near room temperature. Herein, we report a simple, low-energy intensive, and scalable surfactant-assisted reflux method for the synthesis of Sb2Te3 nanoparticles in the solvent ethylene glycol (EG) at low temperatures (120-180 °C). The formation mechanism of platelike Sb2Te3 nanoparticles is proposed. Also, it is found that the size, shape, and chemical composition of the products could be controlled by the introduction of organic surfactants (CTAB, PVP, etc.) or inorganic salts (EDTA-Na2, NaOH, etc.). Additionally, the collected Sb2Te3 nanoparticles were further fabricated into nanostructured pellets using cold-compaction and annealing techniques. Low resistivity [(7.37-19.4) × 10(-6) Ω m], moderate Seebeck coefficient (103-141 μV K(-1)), and high power factor (10-16 × 10(-4) W m(-1) K(-2)) have been achieved in our Sb2Te3-nanostructured bulk materials. The relatively low thermal conductivity (1.32-1.55 W m(-1) K(-1)) is attained in the nanobulk made of PVP-modified nanoparticles, and values of ZT in the range of 0.24-0.37 are realized at temperatures ranging from 50 to 200 °C. Our researches set forth a new avenue in promoting practical applications of Sb2Te3-based thermoelectric power generation or cooling devices.

The tumor microenvironment plays an important role in the tumor's progression and metastasis. Therefore, successful alteration of this delicate setting against the tumor's favor can open a window for therapeutic efficacy. We have developed a modality to bring about treatment-induced alterations in the tumor microenvironment by employing the synergistic effects between two drugs. Co-delivery of rapamycin (RAPA), an mTOR inhibitor that may offer notable therapy through antiangiogenic activity, alongside cisplatin can foster significant potency as RAPA sensitizes A375 melanoma cells to cisplatin therapy through microenvironment modulation. However, encapsulation of these drugs into poly(lactic-co-glycolic acid) (PLGA) NPs was inefficient due to the incompatibility between the two free drugs and the polymer matrix. Here, we show cisplatin can be made hydrophobic by coating a nanoprecipitate (cores) of the drug with dioleoylphosphatidic acid (DOPA). These DOPA coated cisplatin cores are compatible with PLGA and can be coencapsulated in PLGA NPs alongside RAPA at a molar ratio to promote synergistic antitumor activity. The presence of the cisplatin cores significantly improved the encapsulation of RAPA into PLGA NPs. Furthermore, PLGA NPs containing both cisplatin cores and RAPA induced significant apoptosis on A375-luc human melanoma cells in vitro. Additionally, they inhibited the growth of A375-luc melanoma in a xenograft tumor model through modulation of the tumor vasculature and permitted enhanced penetration of NPs into the tumor.

Encapsulation of cisplatin (CDDP) into nanoparticles (NPs) with high drug loading and encapsulation efficiency has been difficult due to the poor solubility of CDDP. However, this barrier has been overcome with a reverse microemulsion method appropriating CDDP's poor solubility to our advantage promoting the synthesis of a pure cisplatin nanoparticle with a high drug loading capacity (approximately 80.8 wt %). Actively targeted CDDP NPs exhibited significant accumulation in human A375M melanoma tumor cells in vivo. In addition, CDDP NPs achieved potent antitumor efficacy through the neighboring effect at a dose of 1 mg/kg when injected weekly via iv without inducing nephrotoxicity. The neighboring effect regards an observation made in vivo when the tumor cells that took up CDDP NPs released active drug following apoptosis. Via diffusion, surrounding cells that were previously unaffected showed intake of the released drug and their apoptosis soon followed. This observation was also made in vitro when A375M melanoma tumor cells incubated with CDDP NPs exhibited release of active drug and induced apoptosis on untreated neighboring cells. However, the neighboring effect was unique to rapidly proliferating tumor cells. Liver functional parameters and H&E staining of liver tissue in vivo failed to detect any difference between CDDP NP treated and control groups in terms of tissue health. By simultaneously promoting an increase in cytotoxicity and a lesser degree of side effects over free CDDP, CDDP NPs show great therapeutic potential with lower doses of drug while enhancing anticancer effectiveness.

Fused-ring and bridged-ring tetrahydrofuran scaffolds are found in a number of natural products and biologically active compounds. A new copper-catalyzed intramolecular carboetherification of alkenes for the synthesis of bicyclic tetrahydrofurans is reported herein. The reaction involves Cu-catalyzed intramolecular addition of alcohols to unactivated alkenes and subsequent aryl C-H functionalization provides the C-C bond. Mechanistic studies indicate a primary carbon radical intermediate is involved and radical addition to the aryl ring is the likely C-C bond-forming mechanism. Preliminary catalytic enantioselective reactions are promising (up to 75% ee) and provide evidence that copper is involved in the alkene addition step, likely through a cis-oxycupration mechanism. Catalytic enantioselective alkene carboetherification reactions are rare and future development of this new method into a highly enantioselective process is promising. During the course of the mechanistic studies a protocol for alkene hydroetherification was also developed.

A new method for the enantioselective synthesis of hexahydro-1H-benz[f]indoles is described. This copper-catalyzed enantioselective intramolecular alkene carboamination process can install vicinal tertiary and quaternary carbon stereocenters with high levels of diastereo- and enantioselectivity. The C-C bond-forming component of the reaction constitutes a C-H functionalization and no electronic activation of the aryl ring that undergoes addition is required. A known 5-HT(1A) receptor antagonist was synthesized efficiently using this method.