发明公开
EP1140832A4 PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES 审中-公开
用于生产ARYLPIPERIDINCARBINOL中间体及其衍生物

PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES
摘要:
A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.
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