3-AMINO-3-ARYLPROPAN-1-OL DERIVATIVE, ITS PRODUCTION AND USE

摘要

PROBLEM TO BE SOLVED: To obtain a new compound effective for painkilling proper for the therapy of pain, and useful as a local anesthetic, an antiarrhythmic agent or the like. SOLUTION: This new compound is the one of formula I (R1 and R2 are each a 1-6C alkyl or form a ring with each other; R3 is a 3-6C alkyl, a 3-6C cycloalkyl or the like; R4 and R5 are each a 1-6C alkyl or the like) in a base or a salt form with a physiologically compatible acid, e.g. 2-(dimethylaminophenylmethyl)-1-(3-methoxyphenyl)cyclohexanol and its hydrochloric acid salt. The compound of formula I is obtained by reacting a Mannich-base of formula II with a nucleophilic reagent (preferably an organometallic compound) at (-70)-110 deg.C. The compound of formula I can be used as a mixture with an antipode, preferably be present at 5-45 wt.% as an active ingredient.