Method for preparing phosphinic acids used in preparing ace...

Details Method for preparing phosphinic acids used in preparing ace... Method for preparing phosphinic acids used in preparing ace...

C - Chemistry, Metallurgy

07

F

260/271.3, 260/3

C07F 9/32 (2006.01)

Patent

CA 1336433

A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula Image wherein R1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl; R2 is hydrogen, lower alkyl or arylalkyl; X is hydrogen, lower alkyl or phenyl; Y is hydrogen, lower alkyl, phenyl or alkoxy, or together X and Y are -(CH2)2-, -(CH2)3-, -CH=CH-, or Image ; and n is 0 or 1 including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure Image wherein R3 is a group removable by hydrogenolysis such as benzyl or substituted benzyl, with a halo ester of the structure Image in the presence of an organic base to form a phosphinic acid ester of the structure Image hydrogenating the above ester to form a diastereomic mixture of a phosphinic acid of the structure Image recrystallizing to recover the preferred racemic mixture and resolving same employing a resolving agent, preferably L-cinchonidine, to form the corresponding resolved salt which may be acidified to the corresponding acid. In addition, novel intermediates which are acids and salts as described above are also provided.

576217

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