The diastereoselective preparation of phosphinate esters

Details The diastereoselective preparation of phosphinate esters The diastereoselective preparation of phosphinate esters

C - Chemistry, Metallurgy

07

F

260/325.1, 260/4

C07F 9/572 (2006.01) C07F 9/32 (2006.01)

Patent

CA 2032900

An increase in the diastereoselectivity resulting from the reaction of a phosphinic acid ester of the formula (see formula I) with the halo ester of the formula (see formula II) is achieved by carrying out the reaction in the presence of 4-methylmorpholine, diazabicyclooctane, quinuclidine, 1-methylpyrolidine, or cinchonidine. After removal of the R3 protecting group and fractional crystallization, the resulting desired diastereomeric pair can be resolved, and the desired isomer can be coupled to 4-substituted L-proline to give compounds possessing angiotensin converting enzyme inhibition activity. In particular, the process is useful in producing the antihypertensive agent fosinopril sodium in increased yields.

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