123599-78-0Relevant articles and documents
PROCESS FOR THE PREPARATION OF FOSINOPRIL AND INTERMEDIATES THEREOF
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Page/Page column 5, (2012/06/16)
The present invention relates to a process for the preparation of intermediates useful in the synthesis of [1[S(R)],2α,4β]-4-cyclohexyl-1-[[[2-methyl-1-oxypropoxy)propoxy](4-phenylbutyl phosphinyl]acetyl]L-proline, and the synthesis thereof, in particular as sodium salt (fosinopril sodium).
Process for the preparation of fosinopril and intermediates thereof
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Page/Page column 7, (2011/01/11)
Process for the preparation of intermediates useful in the synthesis of [1[S(R)],2α,4β]-4-cyclohexyl-1-[[[(2-methyl-1-oxypropoxy) propoxy](4-phenylbutyl) phosphinyl]acetyl]-L-proline, and the synthesis thereof, in particular as sodium salt.
Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby
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, (2008/06/13)
A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula STR1 wherein R 1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl;R 2 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 --(CH 2) 2 --, --(CH 2) 3 --, --CH CH--, or STR2 and n is 0 or 1including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure STR3 wherein R 3 is a group removable by hydrogenolysis such as benzyl or substituted benzyl, with a halo ester of the structure STR4 in the presence of an organic base to form a phosphinic acid ester of the structure STR5 hydrogenating the above ester to form a diastereomic mixture of a phosphinic acid of the structure STR6 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.