Preparation of 4-phenyl-1,2,3,6-tetrahydropyridine

专利名称：Preparation of 4-phenyl-1,2,3,6-tetrahydropyridines

发明人：Francis Brion,Christian Richard申请号：US09/334776申请日：19990616公开号：US06136981A公开日：20001024

摘要：A process for the preparation of a compound of the formula ##STR1## whereinR.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 8 carbonatoms, R.sub.2 and R.sub.4 are alkyl of 1 to 4 carbon atoms and R.sub.3 is alkyl of 1 to 8carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1,R. sub.2, R. sub.3 and R.sub.4 are defined as above or an amine salt thereof with anelectrophilic halogenating agent to obtain a compound of the formula ##STR3## whereinHal.sub.1 is halogen, reacting the latter with a halohydroxylating agent to obtain acompound of the formula ##STR4## wherein Hal.sub.2 is halogen, reacting the latter witha base to obtain a compound of the formula ##STR5## reacting the latter with adiastereoselective reducing agent to obtain a compound of the formula ##STR6##reacting the latter with a reducing agent to obtain a cis racemic compound of formula Iand optionally resolving the latter with a resolution agent to obtain the desired opticalform and novel intermediates.

申请人：HOECHST MARION ROUSSEL

代理机构：Bierman, Muserlian and Lucas

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