A convenient feasible protocol was developed for the preparation of novel tryptamine derivatives from evodiamine. After the general alkylation in N-13 and followed by the treatment of TFA in chloroform, a series of tryptamine derivatives 4a-i were successfully synthesized in a good yield, which were immediately cyclized to form alcohol 5 in the condition of NaOH/methanol.

Hongzhuo Wei, XH Wang, Weihang Guo, Y. H Wang and C. K. Zhao