First Preparative Enantiomer Resolution of Pirlindole, a Potent Antidepressant Drug
作者:
Pascal de Tullio,
Apostolos Felikidis,
Bernard Pirotte,
Jean‐François Liégeois,
Monique Stachow,
Jacques Delarge,
Attilio Ceccato,
Philippe Hubert,
Jacques Crommen,
Joseph Géczy,
期刊:
Helvetica Chimica Acta
(WILEY Available online 1998)
卷期:
Volume 81,
issue 3‐4
页码: 539-547
ISSN:0018-019X
年代: 1998
DOI:10.1002/hlca.19980810307
出版商: WILEY‐VCH Verlag GmbH
数据来源: WILEY
摘要:
AbstractPirlindole is an antidepressant drug. It acts principally as reversible inhibitor of monoamine oxidase‐A (RIMA) and appears relatively potent in comparison with reference drugs. Pirlindole possesses stereogenic center but is generally used as racemate. In this work, the first preparative resolution of its enantiomeric couple is described. Whereas selective crystallization of salts of chiral acid failed, two asymmetric synthetic pathways were also examined; however, without success. Finally separation and isolation of enantiomers of pirlindole was completed by using the derivatization method coupled with preparative HPLC. Optical purity of each isomer was determined by chiral HPLC. The specific rotation of each antipode was also determine
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