Synthesis and anti-depression activity of 3- methyl -5- phenyl -2-( 3- fluorophenyl) morpholine hydrochloride. Fast-paced modern life and mental and psychological pressures have significantly increased the incidence of depression. The treatment of depression includes medication, psychotherapy, physical therapy, crisis intervention and social function rehabilitation, among which medication plays an important role.

With the increasing market scale of antidepressants in the world, developing antidepressants with good curative effect, quick effect and little side effect has become a research hotspot for pharmaceutical workers. Duloxetine, the third generation antidepressant, is an inhibitor of double uptake of 5-HT and NE. Compared with traditional antidepressants, Duloxetine takes effect quickly, and its safety and cure rate are greatly improved. According to the research of N- methylmorpholine manufacturers, 2- arylmorpholine compounds can resist the sedative effect of mice induced by butylenazine, which shows that these compounds have good antidepressant activity.

Therefore, the synthesis of new 2- aryl -2- morpholine compounds with this compound as the lead compound is of great significance for the research of new antidepressant drugs. Boswell et al. used 2- bromoaryl alkyl ketone and 2- amino -1- butanol as raw materials, and reacted in acetonitrile solvent for 72h to obtain 2- aryl -2- morpholinol compounds. After being reduced by NaBH4 for 24h, the ring-opening reaction produces diol compounds, which are dehydrated by concentrated H2SO4 to obtain 3- methyl -5- ethyl -2- phenylmorpholine.

Asselin reported that 2- morpholinol derivatives were synthesized in benzene solution at 80℃ for 20 h. In this paper, based on the previous work of our group, 2- bromo -3'- fluorophenylacetone and phenylaminoethanol were subjected to the nonclassical Leuckart-Wallach reaction, and hydrochloric acid was acidified into salt to obtain a new morpholine hydrochloride compound with 3-methyl and 5-phenyl groups, which shortened the reaction time and achieved ideal yield. According to the pharmacological experimental model of forced swimming in Porsolt mice, the antidepressant activity of the target compound was studied.