| 摘要 |
<p>A process is provided for preparing phosphinic acid prodrug intermediates which are useful in preparing phosphinic acid angiotensin-converting enzyme inhibitors which method includes the step of coupling a phosphonous acid or its ester of the structure <CHEM> wherein R is H or lower alkyl and R<1> is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl, with an alkylating agent of the structure <CHEM> wherein Hal is Cl, Br or I, n is 0 or 1, R<2> is H or lower alkyl, and Z is H, lower alkyl, -CO2R<3> (wherein R<3> is H or lower alkyl, -@-R<4> (wherein R<4> is H, lower alkyl, aryl or arylalkyl), -CN, or <CHEM> (wherein R<5> and R<6> may be the same or different and are selected from the group consisting of H, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkylalkyl and at least one of R<5> and R<6> is other than H, or R<5> and R<6> can be taken with the N-atom to form a 5, 6- or 7-membered heterocyclic ring which 5-, 6- or 7-membered N-containing ring may or may not contain a CO2R<3> group and which 5- or 6-membered N-containing ring may or may not be fused to an aryl ring), in the presence of a silylating agent, to form the phosphinic acid intermediate of the structure <CHEM> wherein R, R<1>, R<2>, n and Z are as defined above. o</p> |
