[EN] STEREOSPECIFIC PROCESS FOR 3-HETEROCYCLYLCYCLOALIPHATIC-1,2-DIOLS<br/>[FR] PROCÉDÉ STÉRÉOSPÉCIFIQUE POUR DIOLS 3-HETEROCYCLYLCYCLOALIPHATIQUES-1,2
申请人:ICAHN SCHOOL OF MEDECINE AT MOUNT SINAI
公开号:WO2017024229A1
公开(公告)日:2017-02-09
A process for the stereoselective synthesis of chiral 3-heterocyclyl-1,2-dihydroxy cyclohexanes is disclosed. The process involves reacting a tricyclic nitrogenous heterocycle with an allyl carbonate in the presence of a chiral palladium catalyst followed by oxidation of the olefinic bond to provide 3-heterocyclyl-1,2-dihydroxy cyclohexanes, cyclopentanes and corresponding alicyclic heterocycles. Also disclosed are methods for converting the heterocyclyl-1,2-dihydroxy cyclohexanes to 2-amino-6-(heteroaryl)cyclohexanols (and related cyclic compounds).