| 摘要 |
The present invention provides a process for the preparation of a compound of formula (II), which comprises condensing a compound of formula (III), wherein R is an acyl group of an alkanoic acid, an aromatic carboxylic acid, an aralkanoic acid, or an alkane- or aromatic-sulfonic acid; with a compound of the formula (IV): NHR<5>R<6>. A particularly preferred ester is the acetate ester. The aminomethyl-phenylimidazoles have useful properties as highly selective partial agonists or antagonists at brain dopamine receptor subtypes. A preferred compound prepared is 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine. Esters of the hydroxymethyl-phenylimidazoles are useful intermediates. |
