【文章名】A Practical Synthesis of [(1S,3S)-3-Aminocyclohexyl]methanol and 2-[(1S,3S)-3-Aminocyclohexyl]propan-2-ol, Useful Intermediates for the Preparation of Novel mPGES-1 Inhibitors
A Practical Synthesis of [(1S,3S)-3-Aminocyclohexyl]methanol and 2-[(1S,3S)-3-Aminocyclohexyl]propan-2-ol, Useful Intermediates for the Preparation of Novel mPGES-1 Inhibitors
作者
WALKER DANIEL P; HEASLEY STEVEN E; MACINNES ALLISON; ANJEH TIZAH; LU HWANGFUN; FOBIAN YVETTE M; COLLINS JOE T; VAZQUEZ MICHAEL L; MAO MICHAEL K
[摘要]:Microsomal prostaglandin E2 synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. During the course of studies aimed at the identification of a suitable mPGES-1 inhibitor for clinical development, a need arose for preparing enantiomerically enriched amino alcohols (S, S)-2 and (S, S)-3. Described herein, a concise synthesis of (S, S)-2 and (S, S)-3 has been developed wherein both amino alcohols are derived from a commercially available, low-cost starting material.