PENICILLOIC ACID DERIVATIVES.

摘要

1,201,977. Penicilloic acid derivatives. F. HOFFMANN-LA ROCHE & CO. A.G. 20 Dec., 1968 [4 Jan., 1968], No. 60560/68. Heading C2C. Novel penicilloic acid derivatives of the formula wherein n is 1 to 4, R1 is hydrogen or C 1 to C 6 acyl, and R is 2-pentenyl; n-pentyl; n heptyl; allylthiomethyl; 5-amino-5-carboxypentyl; benzyl; carboxybenzyl; α-aminobenzyl; phenoxybenzyl; phenbxymethyl; α-phenoxyethyl; α- phenoxypropyl; 2,6-dirnethoxyphenyl; 2-ethoxy-1-naphthyl; 3-carboxy-2-quinoxyalinyl; 5- methyl - 3 - phenyl - 4 - isoxazolyl; 3 - (2 - chlorophenyl) - 5 - methyl - 4 - isoxazolyl; or 3 - (2,6 - dichlorophenyl) - 5 - methyl - 4 - isoxazolyl, and salts thereof, are prepared by reacting a penicillin of formula with a diaminocarboxylic acid derivative of formula R and n being as above and R2 being C 1 to C 6 acyl or an amino-protecting group, (e.g. tert.-butyloxycarbonyl or benzyloxycarbonyl), splitting off the protecting group if present, and optionally converting the reaction product to a salt. The reaction is performed in aqueous alkaline medium. Pharmaceutical compositions comprise the novel penicilloic acids or their pharmaceutically acceptable salts together with a pharmaceutical carrier. The compositions may be in forms for enteral or parenteral administration and are for counteracting allergic reactions produced by administering penicillins.