AN OPTICALLY PURE PIPECOLOXYLIDIDE HYDROCHLORIDE AND A PROCESS FOR ITS PREPARATION

摘要

S- (-)-1- PROPYL- 2', 6'- PIPECOLOXYLIDIDE HYDROCHLORIDE, USED TO INDUCE LOCAL ANESTHESIA, HAS PREVIOUSLY ONLY BEEN KNOWN IN A FORM WHICH IS UNSTABLE AND HYGROSCOPIC, AND WHICH CONTAINS ABOUT 10% BY WEIGHT OF THE MUCH LESS ACTIVE R- (+)- ENANTIOMER. THE PRESENT INVENTION PROVIDES STABLE OPTICALLY PURE S-( - ) -1- PROPYL-2',6'- PIPECOLOXYLIDIDE HYDROCHLORIDE IN THE FORM OF ITS MONOHYDRATE, WITH THE STRUCTURAL FORMULA.( FORMULA I )A PROCESS FOR THE PREPARATION THEREOF BY DISSOLVING THE HYDROCHLORIDE IN WATER, ADDING ACETONE WHICH HAS BEEN HEATED TO A TEMPERATURE OF FROM 45°C TO ITS BOILING POINT, AND ISOLATING THE MONOHYDRATE FORMED AND ITS USED IN INDUCING LOCAL ANESTHESIA.