专利号:US-7259277-B2 优先权日:2003-07-25 标题 :Advanced route for the synthesis of cPLA2 inhibitors 发明人:WU YANZHONG; RAVEENDRATH PANOLIL 权利人:WYETH CORP 摘要:A process for making a compound of formula (I) n nin which process the compound HC≡C—(CH 2 ) n —NH 2 is reacted with the compound R 1 —SO 2 Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formulan n nto produce the compound of formula (I), and compounds produced by the process of this invention. The terms R 1 , R 2 , R 3 , R 4 and n have the definitions set forth in the specification.
专利号:US-7582771-B2 优先权日:2003-09-03 标题:Process for the synthesis of cPLA2 inhibitors 发明人:DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL; REN JIANXIN; WU CHARLES C; WU YANGZHONG 权利人:WYETH CORP 摘要:A process for making the compound of formula (I) n nwherein Ac represents acetate; X represents O or CH 2 ; Y represents C 1 -C 6 alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF 3 , OCF 3 , OH, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkyl, NH 2 , N(C 1 -C 6 alkyl) 2 , NH(C 1 -C 6 alkyl), NC(O)—(C 1 C 6 alkyl), and NO 2 . In his process, a compound of formula (II)n n nis reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
专利号:US-7342119-B2 优先权日:2003-09-30 标题 :Process for the synthesis of a CPLA2 inhibitor 发明人:DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL 权利人:WYETH CORP 摘要:A process for making a substituted indole compound, including the steps of: reacting the compounds n nin a non-protic polar solvent in the presence of a catalyst to form the intermediate compoundn n nwherein Ph and X are as defined herein; and then,n nheating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compoundn n nThe invention also includes compounds formed by this process.
专利号:US-2005049296-A1 优先权日:2003-09-03 标 题 :Process for the synthesis of cPLA2 inhibitors
专利号:US-2008177085-A1 优先权日:2003-09-30 标 题:Process for the Synthesis of a CPLA2 Inhibitor
专利号:US-2005070723-A1 优先权日:2003-09-30 标 题 :Process for the synthesis of a CPLA2 inhibitor
参考标题:Practical Highly Enantioselective Synthesis Of Propargylamines Through A Copper-Catalyzed One-Pot Three-Component Condensation Reaction 作者:Nina Gommermann,Paul Knochel |发布日期:2006.5.24 摘要:The One-Pot Three-Component Reaction Of Terminal Alkynes, Aldehydes And Secondary Amines In The Presence Of Copper(I) Bromide/quinap Is Reported. The Reaction Scope Has Been Determined And A Broad Variety Of All Three Components Has Been Used, Which Afforded The Corresponding Propargylamines In Good To Excellent Yields And Moderate To Very Good Enantioselectivities. The Reaction Showed A Strong Positive
合成参考文献
摘要:Le Bras, J.; Muzart, J., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 170.