PREPARATION OF 2-BENZOYLALKYLBENZOMORPHAN

摘要

A novel process for preparing 2-benzoylalkylbenzomorphan derivatives and salts thereof, represented by the formula WHEREIN N, R, R1, R2, R3 and R4 are as defined in the specification. The process comprises reacting a pyridinium derivative of the formula, WHEREIN X is a halogen atom and Y' is an ethylenedioxy group; with a Grignard reagent of the formula, WHEREIN R' is a hydrogen atom or a C1-C3 alkoxy group and Z is a halogen atom, to yield a 1,2-dihydropyridine derivative of the formula; AND THEN REDUCING THE SAID 1,2-DIHYDROPYRIDINE DERIVATIVE TO GIVE A 1,2,5,6-TETRAHYDROPYRIDINE DERIVATIVE OF THE FORMULA, WHEREIN Y is an oxygen atom or an ethylenedioxy group, and further cyclizing the obtained 1,2,5,6-tetrahydropyridine derivative.