Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors

摘要

Preparation of aminocarbonyl derivatives of geneseroline (I) comprises oxidation of eserine, followed by hydrolysis to geneseroline, without isolating the intermediate geneserine, followed by acylation of geneseroline with an isocyanate and optional conversion to a salt. - Preparation of aminocarbonyl derivatives of geneseroline of formula (I) comprises: (a) oxidation of eserine with hydrogen peroxide in the presence of a base; (b) hydrolysis of the intermediate geneserine without isolation to give geneseroline; (c) acylation geneseroline with an isocyanate of formula R-N=C=O in the presence of a basic catalyst; and (d) optionally conversion into a salt. R = 2-20C alkyl, 3-7C cycloalkyl, phenyl or benzyl optionally substituted by 1-4C alkyl, halo or 1-4C alkoxy.