Optimization of synthetic technological conditions for 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hydrochloride with orthogonal design

Abstract:

Objective：To optimize the synthetic technological conditions of 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hy－drochloride as important intermediate for drugs by orthogonal experimental method. Methods：The target product was synthesized from β-phenethylamine by phthalimide N-hydrocarbylation reaction，Bischler-Napieralski reaction，cyclization with Bischler-Napieralski method，hydrazinolysis reaction，reduction and salification. The key factors on each reaction were discussed separately and optimized by orthogonal experiment. Results：The overall yield was 65%，2.5 times as much as that of the reported. Conclusion: The optimized synthetic route has promise in industrial production for its cheap and readily available raw materials，easy and environmentally-friend processes，high yield and good quality of products.