Process for preparing phosphinic acid intermediates

Details Process for preparing phosphinic acid intermediates Process for preparing phosphinic acid intermediates

C - Chemistry, Metallurgy

07

F

260/284, 260/316

C07F 9/30 (2006.01) C07F 9/32 (2006.01) C07F 9/572 (2006.01) C07F 9/60 (2006.01) C07F 9/62 (2006.01)

Patent

CA 1258458

ABSTRACT PROCESS FOR PREPARING PHOSPHINIC ACID INTERMEDIATES 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 Image wherein R is H or lower alkyl and R1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl- alkyl, with a conjugated compound of the structure Image wherein R2, R3 and R4 may be the same or different and each is independently H, lower alkyl or aryl.and Z is lower alkyl, -CO2R5 (wherein R5 is H or lower alkyl), Image (wherein R6 is H, lower alkyl aryl or arylalkyl). -CN, Image (wherein R6 and R8 are 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 R7 and R8 is other than H, or R7 and R8 can be taken together with N to form a 5-, 6- or 7-membered heterocyclic ring Image , which may or may not include a COOR5 substituent, 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 phosphonic acid intermediate of the structure Image wherein R, R1, R2, R3 and R4 and Z are as defined above.

463513

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