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

Patent

CA 1258457

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 an alkylating agent of the structure Image wherein Hal is Cl, Br or I, n is 0 or 1, R is H or lower alkyl, and Z is H, lower alkyl, -CO2R3 (wherein R3 is H or lower alkyl), Image (wherein R4 is H, lower alkyl, aryl or arylalkyl), -CN, or Image (wherein R5 and R6 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 R5 and R6 is other than H, or R5 and R6 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 CO2R3 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 Image wherein R, R1, R2, n and Z ace as defined above.

463512

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