Title:
【発明の名称】ホスフィン酸エステルのジアステレオマー選択的製造法
Document Type and Number:
Japanese Patent JP2846484
Kind Code:
B2
Abstract:
An increase in the diastereoselectivity resulting from the reaction of a phosphinic acid ester of the formula with the halo ester of the formula 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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Inventors:
TOOMASU SHII SEDAAGURAN
Application Number:
JP1946891A
Publication Date:
January 13, 1999
Filing Date:
January 18, 1991
Export Citation:
Assignee:
BURISUTORU MAIYAAZU SUKUIBU CO
International Classes:
A61P9/12; C07F9/32; C07F9/572; A61K31/66; (IPC1-7): C07F9/32; C07F9/572
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)