Indolyl - (3) - malonate and method for their preparation

摘要

1,167,419. Indole derivatives. MERCK & CO. Inc. 16 Aug., 1967 [23 Aug., 1966], No. 37637/67. Heading C2C. 1 - p - Chlorobenzoyl - 2 - methyl - 5 - methoxy- 3-indolylacetic acid is prepared by simultaneous de-esterification and decarboxylation, e.g. by means of hydrolysis or hydrogenolysis in the presence of a hydrolysing agent, of an indole- 3-malonic acid ester of the general formula wherein R is t-butyl or benzyl. Novel indole-3-malonic acid esters of the general formula above are prepared by treatment of an indole-3-malonic acid ester of the general formula with p-chlorobenzoyl chloride. Indole-3-malonic acid esters of the second general formula above are prepared by reaction of p-methoxyphenylhydrazine hydrochloride with 2-acetonyl malonic acid dibenzyl or di-tbutyl ester.