Search

HIV-1 integrase (IN) is a key enzyme in viral replication that catalyzes the covalent integration of viral cDNA into the host genome. Currently, five HIV-1 IN strand transfer inhibitors (INSTIs) are approved for clinical use. These drugs represent an important addition to the armamentarium for antiretroviral therapy. This review briefly illustrates the development history of INSTIs. The characteristics of the currently approved INSTIs, as well as their future perspectives, are critically discussed.

Organic nanotubes have been assembled from pillar[5]arenes 1 and 2. Compound 1 gelates organic solvents through the formation of tubular fibers which are evidenced by TEM and XRD experiments, while 2 assembles into two different channels under the template effect of water wires. In addition, the water wires in the nanotubes of 2 can be under selective proton conductance. The results described herein represent a new strategy for building tubular structures.

An efficient oxidative cyclization of amidoalkylation adducts of activated methylene compounds with the combination of iodosobenzene and a catalytic amount of tetrabutylammonium iodide under neutral conditions is reported. The reaction affords N-benzoyl aziridines or oxazolines in moderate to excellent yields.

The aziridination of alkenes with the direct use of p -toluenesulfonamide (TsNH 2 ) was achieved by using PhI(OAc) 2 and I 2 under mild conditions. The reaction affords aziridines in moderate to good yields, and offers good manipulability by avoiding the use of the expensive metal catalyst and the unstable and explosive PhI NTs.

(Diacetoxyiodo)benzene (PhI(OAc) 2 ) was found to be a powerful reagent to induce the intramolecular oxidative bromocyclization of homoallylic sulfonamides utilizing KBr as the bromine source. The reaction affords 2-substituted-4-bromo-pyrrolidines in moderate to excellent yields under a mild metal-free condition, and offers good manipulability by avoiding the use of highly toxic and caustic bromine (Br 2 ).

A selective β-fragmentation of homoallylamines with the combination of iodobenzene diacetate, iodine, and sodium acetate is reported. The desired carbon–carbon bond cleavage proceeded via a radical β-scission pathway under mild conditions with good functional group tolerance.

A Dy(OTf)3-mediated selective substitution reaction of N-(α-benzotriazolyl-alkyl)amides with active methylene compounds is reported. The present procedure provides a facile method for the synthesis of benzotriazole derivatives.

A highly efficient and practical route to 3-amino-4-sulfanylcoumarins from 3-bromo-4-tosyloxy-coumarins via substitution and palladium catalyzed amination reactions is described.