Process of preparing carboxyalkyl dipeptides

C - Chemistry – Metallurgy – 07 – F

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260/446.6

C07F 7/10 (2006.01) C07F 7/18 (2006.01) C07K 1/08 (2006.01)

Patent

CA 1304388

ABSTRACT OF THE DISCLOSURE Pharmaceutically active carboxyalkyl dipeptides such as enalapril, lisinopril and the like, are prepared from a starting amino acid such as L-alanine, by protecting the acid function of the amino acid with an alkyl silyl protecting group, whilst it is reacted with an .alpha.-halo ester, at its amino function. Subsequently, the silyl protectant is removed, and the acid group is reacted with the amino function of an appropriate amino acid such as L- proline, to form the dipeptide product.

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