Patent ID: 6124503
Filing Date: 2000-09-26
Classification: C07C

Abstract:
A method of making an alkylaminoarylcarbonyl compound having Formula I: ##STR21## wherein R is an alkyl, cycloalkyl or arylalkyl group;A is a phenyl or naphthyl ring;each R' is independently an alkyl group which may form a ring with Z or Z';p is 0, 1, 2, or 3;each Z, Z', and Y is independently hydrogen or an alkyl, cycloalkyl or arylalkyl group; andn is 0, 1, or 2;comprising:(a) blocking the carbonyl function of an aminoarylcarbonyl compound of the formula: ##STR22## via condensation with an active methylene compound of formula: ##STR23## wherein each E' and E"" is independently a cyano, acetate, malonate, formic acid or formate group;whereby there results a blocked aminoarylcarbonyl compound of formula: ##STR24## (b) alkylating this blocked amniocarbonyl compound via reductive alkylation with an alkyl or aryl carbonyl compound to give a blocked alkylaminoarylcarbonyl compound of formula: ##STR25## (c) deblocking of the blocked alkylaminoarylcarbonyl compound via base hydrolysis to regenerate the carbonyl function and give the desired alkylaminoarylcarbonyl compound.