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

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.