专利号:US-8329905-B2 优先权日:2006-06-30 标 题 :Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 发明人:YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K 权利人:YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K; MERCK SHARP & DOHME 摘要:This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: n nwherein R 9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R 11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X 2 is Cl, Br, or I; X 3 is selected from Cl and Br; and PdL n is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
专利号:US-2008004449-A1 优先权日:2006-06-30 标题:Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
专利号:US-8258319-B2 优先权日:2005-01-14 标 题:Exo- and diastereo- selective synthesis of himbacine analogs
专利号:US-2011251392-A1 优先权日:2005-01-14 标 题:Exo- and diastereo- selective synthesis of himbacine analogs
专利号:US-7687631-B2 优先权日:2006-06-30 标 题 :Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
专利号:US-2012296093-A1 优先权日:2005-01-14 标题 :Exo- and diastereo- selective synthesis of himbacine analogs