- Improved large-scale synthesis of(R)-benzyl 4-hydroxyl-2-pentynoate from (R)-3-butyn-2-ol
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A reliable one-pot process for the title compound has been developed for large-scale productions. The effect of reaction conditions such as temperature, order of addition, and amount of the lithiation reagent has been extensively investigated, giving rise to an optimal process with highest attainable yield.
- Fu, Xiaoyong,Yin, Jianguo,Thiruvengadam,McAllister, Timothy L.,Tann, Chou-Hong,Colon, Cesar
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Read Online
- Thrombin Receptor Antagonists Based On The Modified Tricyclic Unit Of Himbacine
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Multiple stereoisomers of the heterocyclic-substituted tricyclics of the formula: or a pharmaceutically acceptable salt, solvate, or ester of said compound wherein R and the stereochemistry are illustrated in the structural formulas herein are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
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Page/Page column 34-35
(2008/06/13)
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- Metabolism-based identification of a potent thrombin receptor antagonist
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The metabolism of our prototypical thrombin receptor antagonist 1, K i = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The structures of the metabolites were verified independently by synthesis. Compound 4 was shown
- Clasby, Martin C.,Chackalamannil, Samuel,Czarniecki, Michael,Doller, Dario,Eagen, Keith,Greenlee, William,Kao, Grace,Lin, Yan,Tsai, Hsingan,Xia, Yan,Ahn, Ho-Sam,Agans-Fantuzzi, Jacqueline,Boykow, George,Chintala, Madhu,Foster, Carolyn,Smith-Torhan, April,Alton, Kevin,Bryant, Matthew,Hsieh, Yunsheng,Lau, Janice,Palamanda, Jairam
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p. 129 - 138
(2008/02/03)
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- Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents
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Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a Ki of 2.7 nM in the binding assay, making it the most po
- Chackalamannil, Samuel,Xia, Yan,Greenlee, William J.,Clasby, Martin,Doller, Darìo,Tsai, Hsingan,Asberom, Theodros,Czarniecki, Michael,Ahn, Ho-Sam,Boykow, George,Foster, Carolyn,Agans-Fantuzzi, Jacqueline,Bryant, Matthew,Lau, Janice,Chintala, Madhu
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p. 5884 - 5887
(2007/10/03)
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