Patent ID: 6211386
Filing Date: 2001-04-03
Classification: A61P,C07D

Abstract:
A process for the preparation of a compound of the formula: ##STR19##where R.sub.3 is selected from the group consisting of:--NO.sub.2,--NH.sub.2,--NH--SO.sub.2 -[4-trifluoromethylpyridin-2-yl],--N(--CH.sub.2 -.phi.).sub.2,--N(R.sub.3-1)(R.sub.3-2) where R.sub.3-1 and R.sub.3-2 are the same or different and are:--H,--CO--O--(t-butyl),--CO--O--CH.sub.2 -.phi.,--CO--CH.sub.3,--CO-.phi.,--Cl,--Br,--I,--OH,--O--SO.sub.2 --CF.sub.3,where n is 0 or 1 with the provisos, (1) that when n is 0 the R.sub.3 group must be in the meta position and (2) that when n is 1, one of R.sub.3 must be --Cl, --Br, --I, --OH or --O--SO.sub.2 --CF.sub.3, where R.sub.4 is selected from the group consisting of --H and --Si(CH.sub.3).sub.3, which comprises hydrogenating a compound of the formula: ##STR20##the E-geometrical isomer thereof or a mixture of the Z- and E-isomers, where R.sub.3 and R.sub.4 are as defined above, in the presence of catalyst containing Rh, a chiral ligand with at least one phosphorous atom where the hydrogenation is conducted in the presence of a base.