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3. ChemInform Abstract: Developments in Factor Xa Inhibitors for the Treatment of Thromboembolic Disorders

Author

Yu-Kai Lee and Mark R. Player

Subjects
medicine.drug_mechanism_of_action, Chemistry, Factor Xa Inhibitor, Advanced stage, General Medicine, Pharmacology, Thrombin, Coagulation, Coagulation cascade, Antithrombotic, medicine, Effective treatment, Discovery and development of direct thrombin inhibitors, medicine.drug
Abstract

Thromboembolic diseases are the leading causes of morbidity and mortality in the developed world. Anticoagulants provide effective treatment for venous or arterial thromboembolism. Two coagulation factors, factor Xa (fXa) and thrombin, are the primary targets under active investigation for anticoagulant therapy. fXa, in contrast to the multifunctional roles of thrombin in the coagulation cascade, converts prothrombin to thrombin collectively at the junction of the intrinsic and extrinsic pathway of coagulation. The effectiveness of fXa inhibitors as antithrombotic agents and their potentially reduced bleeding risks may offer superior therapeutic profiles with respect to thrombin inhibitors. After decades of research, many fXa inhibitors are now in the advanced stages of clinical trials. Unlike most reviews, which only provide incremental updates, this review provides an overview of fXa and the medicinal chemistry of its inhibitors. Overviews on coagulation models, antithrombotic therapy, and fXa will be provided, followed by the evolution of the medicinal chemistry of fXa inhibitors over the past few decades. © 2009 Wiley Periodicals, Inc. Med Res Rev, 31, No. 2, 202–283, 2011

Published
2011

4. ChemInform Abstract: Alkyne-Mediated Domino Hydroformylation/Double Cyclization: Mechanistic Insight and Synthesis of (.+-.)-Tashiromine

Author

Guei-Tang Chen, Yi-Huei Lin, Chien-Lun Kao, Wen-Hua Chiou, Yu-Che Tseng, Jui-Chi Tsai, and Yu-Kai Gao

Subjects
chemistry.chemical_classification, chemistry.chemical_compound, chemistry, Cascade reaction, Alkyne, Indolizidine, Reactivity (chemistry), General Medicine, Selectivity, Carbonylation, Combinatorial chemistry, Hydroformylation, Domino
Abstract

A novel domino reaction, alkyne-mediated domino hydroformylation/double cyclization, has been developed for rapid preparation of indolizidine type alkaloids. DFT calculations were applied for rationales of reactivity and selectivity. A concise synthesis of tashiromine as the application of the methodology is also reported.

Published
2011

6. ChemInform Abstract: Chiral Acetylenic Sulfoxide in Enantioselective Synthesis of Tetrahydroisoquinoline and Tetrahydro-β-carboline Alkaloids. Total Synthesis of (R)-(+)-Carnegine and (R)-(+)-Tetrahydroharman

Author

Wing Hong Chan, Yi Tao, Albert W. M. Lee, and Yu Kai Lee

Subjects
Tryptamine, chemistry.chemical_compound, chemistry, Stereochemistry, Tetrahydroisoquinoline, Alkaloid, Michael reaction, Enantioselective synthesis, Total synthesis, Sulfoxide, General Medicine, Ethylamine
Abstract

Michael addition of 2-(3,4-dimethoxyphenyl)ethylamine 3 or tryptamine 4 onto chiral acetylenic sulfoxides 2 followed by acid induced cyclization afforded the basic alkaloid skeleton of tetraisoquinoline and tetrahydro-β-carboline in high to moderate diastereoselectivity. Optically pure (R)(+)-Carnegine and (R)-(+)-tetrahydroharman have been synthesized.

Published
2010

7. ChemInform Abstract: Intramolecular Diels-Alder Reactions of Vinylboranes. A Highly Stereoselective Two-Step Decalin Synthesis

Author

Daniel A. Singleton and Yu-Kai Lee

Subjects
Hydroboration, chemistry.chemical_compound, Decalin, Chemistry, Intramolecular force, Two step, Diels alder, Organic chemistry, Stereoselectivity, General Medicine
Abstract

1,7,9-Decatrienylboranes, generated in situ from either hydroboration of 5 or boron-tin exchange with 6 , undergo very highly stereoselective intramolecular Diels-Alder reactions.

Published
2010

8. ChemInform Abstract: Catalysis by Temporary Covalent Activation. A Novel Catalysis of Unactivated Diels-Alder Reactions

Author

Jose P. Martinez, Daniel A. Singleton, Yu-Kai Lee, and S.‐W. Leung

Subjects
Hydroboration, Covalent bond, Chemistry, Diels alder, Organic chemistry, General Medicine, Catalysis
Abstract

Diels-Alder reactions of cis-2-chlorovinyltributylstannane are greatly accelerated by the presence of catalytic amounts of haloboranes. Mechanistic studies support a mechanism for the catalysis involving an intermediate boron-activated dienophile. A similar but simpler catalysis of Diels-Alder reactions of unactivated alkynes, via a hydroboration — Diels-Alder — dehydroboration mechanism, is also described.

Published
2010

39. ChemInform Abstract: Assembly of Sandwich-Type 3-D Supramolecular Coordination Polymers Based on Hexa-Molybdenum Chain and {PMo12O40} Heteropolyanion.

Author

Wan, Siqi, Yu, Kai, Wang, Lu, Su, Zhanhua, and Zhou, Baibin

Subjects
*MOLYBDENUM compounds, *HETEROCHAIN polymers, *SUPRAMOLECULAR polymers, *ORTHORHOMBIC crystal system, *RHODAMINE B
Abstract

Yellow block crystals of H3O[Mo6(bipy)6O17] [PMo12O40]·2H2O are hydrothermally synthesized from a mixture of H3PMo12O40, Ba(NO3)2, bipy, HNO3, and H2O (autoclave, pH 2.0, 170 °C, 3 d; 40% yield). [ABSTRACT FROM AUTHOR]

Published
2016
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40. ChemInform Abstract: Organic-Inorganic Hybrid Materials Based on Basket-Like {Ca@P6Mo18O73} Cages.

Author

Zhang, He, Yu, Kai, Lv, Jing‐hua, Gong, Li‐hong, Wang, Chun‐mei, Wang, Chun‐xiao, Sun, Di, and Zhou, Bai‐Bin

Subjects
*ORGANIC compounds, *INORGANIC compounds, *HYDROTHERMAL synthesis, *SINGLE crystals, *X-ray diffraction, *CALCIUM, *COPPER
Abstract

Compounds (IV), (VI), (VII), and (VIII) are hydrothermally synthesized and their structures are determined by single crystal XRD. [ABSTRACT FROM AUTHOR]

Published
2015
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41. ChemInform Abstract: The Highest Connected Pure Inorganic 3D Framework Assembled by {P4Mo6} Cluster and Alkali Metal Potassium.

Author

Zhang, He, Yu, Kai, Li, Jingshen, Wang, Chunmei, Lv, Jinghua, Chen, Zhaoyi, Cai, Honghong, and Zhou, Baibin

Subjects
*MOLYBDENUM, *POTASSIUM, *X-ray diffraction, *POLYOXOMETALATES, *NITRITES, *HYDROGEN peroxide, *VITAMIN C
Abstract

Dark-blue crystals of [K(H2O)]12 [CoMo12O24(OH)6 (HPO4)4(PO4)4] are hydrothermally prepared from a mixture of (NH4)6Mo7O24, Co(AcOH)2, KOAc, bipy, H3PO4, NaOH, and H2O (autoclave, pH 3.5, 160 °C, 4 d, 46% yield). [ABSTRACT FROM AUTHOR]

Published
2015
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