TRANS-(-)-4-(4-FLUOROPHENYL)-3-HYDROXYMETHYLPIPERIDINE L-TARTRATE AND ITS PRODUCTION

摘要

PROBLEM TO BE SOLVED: To obtain a new compound useful as an intermediate for paroxetine usable as an antidepressant and the like and capable of being efficiently obtained by using an inexpensive optical resolution agent. SOLUTION: This compound is a trans-(-)-4-(4-fluorophenyl)-3- hydroxymethylpiperidine L-tartrate of formula I (R1 is H, an 1-6C alkyl or 7-12C aralkyl), e.g. transm-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine L-tartrate. The compound of formula I is obtained by subjecting trans-(±)-4-(4- fluorophenyl)-3-hydroxymethylpiperidines to salt-formation with L-tartaric acid by using pref. a solvent (e.g. a methanol solvent or mixture solvent of methanol and at least one of isopropyl alcohol and acetone) containing methanol as a main component, which leads to expect that the objective compound may be obtained in high yield by an inexpensive optical resolution agent.