发明名称 PROCESS FOR PREPARING ALPHA-CARBOXAMIDE DERIVATIVES
摘要 The present application provides a process for the preparation ofα-carboxamide pyrrolidine derivatives of formula (I), wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or such R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; either R6 or R7 is—O—R8,—OCHR9R8,—NCH2R8 or—(CH2)2R8 wherein the other R6 or R7 is hydrogen or R5; and wherein R8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and R9 is hydrogen or C1-3alkyl.
申请公布号 US2012226053(A1) 申请公布日期 2012.09.06
申请号 US201013393174 申请日期 2010.09.01
申请人 ZAJAC MATTHEW ALLEN;CONVERGENCE PHARMACEUTICALS LIMITED 发明人 ZAJAC MATTHEW ALLEN
分类号 C07D207/09 主分类号 C07D207/09
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