Patent ID: 6586634
Filing Date: 2003-07-01
Classification: A61P,C07B,C07C

Abstract:
A process for the preparation of (1S,2R)-1-amino-2-indanol-(R,R)-tartrate methanol solvate comprising:reacting in a solvent a mixture of enantiomers of cis-1-amino-2-indanol at an elevated temperature with (R,R)-tartaric acid and methanol to form a reaction mixture, such that (1S,2R)-1-amino-2-indanol is present at a concentration of 0.02 g-0.1 g per ml of solvent; crystallizing optically enriched (1S,2R)-1-amino-2-indanol-(R,R)-tartrate methanol solvate from the reaction mixture; and recovering crystals of (1S,2R)-1-amino-2-indanol-(R,R)-tartrate methanol solvate at a temperature between 10Â° C. and 50Â° C. in the presence of 0-20 wt. % water relative to the amount of methanol plus solvent, wherein the recovery takes place at a temperature between 30Â° C. and 50Â° C. if the reaction mixture is essentially free from water and wherein (1S,2R)-1-amino-2-indanol-(R,R)-tartrate is recovered in an enantiomeric excess of greater than 96% relative to (1R,2S)-1-amino-2-indanol-(R,R)-tartrate.