摘要 |
<p>A process for the preparation of compounds of formula (I), wherein R is C2-C20 linear or branched alkyl, C3-C7 cycloalkyl, phenyl or benzyl, which can optionally be substituted by C1-C4 alkyl, halogen or C1-C4 alkoxy group, said process comprising: a) oxidation of eserine with hydrogen peroxide in the presence of a base and subsequent hydrolysis to geneseroline, without isolating the intermediate geneserine; b) acylation of geneseroline with an isocyanate of formula R-N=C=O, wherein R is as defined above, in the presence of a basic catalyst; c) optional transformation into a pharmaceutically acceptable salt. Compounds of formula (I) wherein R is a phenyl or benzyl, which can be optionally substituted by alkyl, halogen or alkoxy, are selective, potent brain anticholinesterase inhibitors.</p> |
申请人 |
CHIESI FARMACEUTICI S.P.A.;CHIESI, PAOLO;VENTURA, PAOLO;SERVADIO, VITTORINO;PIGHI, ROBERTO;PIVETTI, FAUSTO;SALSI, BLUETTA;DELCANALE, MAURIZIO;AMARI, GABRIELE;PIETRA, CLAUDIO;VILLETTI, GINO |
发明人 |
CHIESI, PAOLO;VENTURA, PAOLO;SERVADIO, VITTORINO;PIGHI, ROBERTO;PIVETTI, FAUSTO;SALSI, BLUETTA;DELCANALE, MAURIZIO;AMARI, GABRIELE;PIETRA, CLAUDIO;VILLETTI, GINO |