PROCESSES FOR PRODUCING (AMINOMETHYL)TRIFLUOROCARBINOL DERIVATIVES

摘要

The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives (I), in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc. The present invention relates to a process for producing the compound (I) from 1,3-oxazolidin-5-one derivative (II) being easily derived from an alpha -amino acid, which is carried out stepwise or by one-spot reaction, and further relates to a process for producing the compound (I) comprising the reduction of the 5-hydroxy compound (II). wherein R<1> is a group corresponding to the side chain of a natural or non-natural alpha -amino acid, R<2> is a hydrogen atom or R<21> (in which R<21> is a protecting group for amino group having a carbonyl group at the binding site to the nitrogen atom).