Preparation method of (S)-3-methylamino-1-(2-thienyl)-1-propanol

Abstract

The invention relates to a preparation method of (S)-3-methylamino-1-(2-thienyl)-1-propanol. (S)-3-dimethylamino-1-(2-thienyl)-1-propanol is used as a raw material to be treated by the following stepsof (1) performing hydroxy group protective reaction on the (S)-3-dimethylamino-1-(2-thienyl)-1-propanol; (2) performing demethylation reaction; (3) performing hydroxy removal reaction protection. Thepreparation method has the advantages that the reaction byproducts are few; the purity is high; the reaction speed is high; the yield is high.

Description

technical field [0001] The present invention specifically relates to a preparation method of (S)-3-methylamino-1-(2-thienyl)-1-propanol. Background technique [0002] (S)-3-Methylamino-1-(2-thienyl)-1-propanol is an important intermediate of the antidepressant duloxetine. Duloxetine is a safe and effective antidepressant developed by Eli Lilly and Company (Elilly), and it is a dual reuptake inhibitor of serotonin and norepinephrine. With the increasing number of depressed people in the world, the demand for antidepressants with high efficacy and low toxicity is increasing. Compared with other antidepressants, such as paroxetine, fluoxetine and reboxetine, duloxetine has better safety and tolerance, fewer adverse reactions, and has diverse therapeutic activities, so The sales volume has increased year by year [1], and now it occupies the first place in the global sales list of antidepressants. For this reason, many researchers are devoted to the exploration of the syntheti...

AI Technical Summary

Problems solved by technology

The production and preparation methods in the prior art are inefficient, and there are many by-products in the prepared products, making purification difficult