Process for the preparation of lower alkyl esters of...

Details Process for the preparation of lower alkyl esters of... Process for the preparation of lower alkyl esters of...

C - Chemistry, Metallurgy

07

K

530/5.06

C07K 5/06 (2006.01) C07K 5/075 (2006.01)

Patent

CA 1212940

ABSTRACT OF THE DISCLOSURE The invention relates to a selective process for the preparation of N-L-.alpha.-aspartyl-L-phenylalanine-1-lower alkyl ester which comprises: A. reacting an L-aspartic acid 4-arylmethyl ester with a i) 1,3-diketone; or ii) acylacetic ester; in the presence of a base to form the salt of i') L-N-(1-alkyl-2-acyl-vinyl)-aspartic acid 4-arylmethyl ester; or ii') L-N-(1-alkyl-2 alkoxycarbonyl-vinyl)-aspartic acid 4-arylmethyl ester, and then either: 1) reacting salt (i') or (ii') with an organic or in- organic acid halide having the formula X-A, wherein X represents a halogen and A has the meaning indicated hereinafter, or with an acid anhydride to form Image I wherein R represents an alkyl radical with 1 to 6 carbon atoms; R' represents an alkyl or alkoxy radical with 1 to 6 carbon atoms; Ar represents the phenyl, nitrophenyl, halogenphenyl or alkylphenyl radical; and

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