发明名称 |
A PROCESS FOR THE PREPARATION OF AMINOCARBONYL DERIVATIVES OF GENESEROLINE HAVING SELECTIVE BRAIN ANTICHOLINESTERASE ACTIVITY |
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> |
申请公布号 |
CA2274658(A1) |
申请公布日期 |
1999.04.22 |
申请号 |
CA19982274658 |
申请日期 |
1998.10.07 |
申请人 |
CHIESI FARMACEUTICI S.P.A. |
发明人 |
PIETRA, CLAUDIO;SERVADIO, VITTORINO;AMARI, GABRIELE;SALSI, BLUETTA;CHIESI, PAOLO;VILLETTI, GINO;DELCANALE, MAURIZIO;VENTURA, PAOLO;PIGHI, ROBERTO;PIVETTI, FAUSTO |
分类号 |
C07D498/04;(IPC1-7):C07D498/04;A61K31/535;C07D487/04 |
主分类号 |
C07D498/04 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|