SYNTHESIS OF FATTY ALCOHOL ESTERS OF A-HYDROXY CARBOXYLIC ACIDS AND THEIR USE AS PERCUTANEOUS ABSORPTION ENHANCERS

摘要

The present invention provides a novel approach for the preparation of fatty alcohol esters ofα-hydroxy carboxylic acids. In one form of the invention, the target fatty alcohol ester ofα-hydroxy carboxylic acid is produced by converting a lower alkyl ester ofα-hydroxy carboxylic acid into a fatty alcohol ester ofα-hydroxy carboxylic acid via alcoholysis (i.e., transesterification). The transesterification process is an equilibrium reaction, catalyzed chemically (i.e., with acids or bases) or enzymatically, that is shifted in the desired direction to produce the desired product. One preferred way of shifting the reaction in the direction of the desired product is by reducing the concentration of one of the products (e.g., distillation of a lower-boiling alcohol as soon as it is formed). Another preferred way of shifting the reaction in the direction of the desired product is by increasing the concentration of one of the reactants (e.q., adding more of the starting ester).