Process for the preparation of 2-(2-thenyl)-1,4,5-trimethyl-1,2,3,6-tetrahydropyridine and use of the latter for the preparation of 2,4,5-trimethylthieno[3,2-f]morphane

摘要

2-Cyano-4,5-dimethylpyridine is reacted with an ether solution of thienyllithium, and by acid hydrolysis 2-thienyl 4,5-dimethyl-2-pyridyl ketone is obtained; by heating in the presence of hydrazine hydrate in basic medium, a 2-(2-thenyl)-4,5-dimethylpyridine is obtained which by heating in the presence of methyl iodide gives an intermediate product which is purified with NaBH4 in ethanol to produce 2-(2-thenyl)-1,4,5-trimethyl-1,2,3,6-tetrahydropyridine; by heating this body in the presence of HB2 the 2,4,5-trimethyl-thienomorphane of the formula below is obtained. Pharmaceutical application as an analgesic. <IMAGE>