US 2022/0024860 A1 · METHOD FOR CONTINUOUSLY PREPARING CITALOPRAM DIOL

Abstract

The present application relates to a method for citalopram intermediate citalopram diol. The method comprises: first mixing two Grignard reagents required for a reaction; then mixing the mixed Grignard reagents with a raw material 5-cyanophthalide in a temperature-controllable micromixer to obtain a reaction solution; then subjecting the reaction solution to the reaction by means of a reactor to obtain a citalopram diol reaction solution; and then performing operations such as quenching, concentration, extraction, acidification, and crystallization to obtain a qualified product. The citalopram diol provided in the present invention has good selectivity, high yield, high safety, safety and reliability, and little sewage discharge, and is suitable for industrial production.

Claims20

Dependent claims

A method for continuously preparing citalopram diol or a citalopram diol salt, comprising:

(1) preparing an organic solvent feed liquid A containing 5-cyanophthalide of formula 2;
(2) preparing a mixed feed liquid B containing Grignard reagent of formula 3 and Grignard reagent of formula 4;
(3) mixing the organic solvent feed liquid A in step (1) with the mixed feed liquid B in step (2) by a temperature-controllable micromixer to obtain a reaction solution C;
(4) reacting the reaction solution C in a reactor to obtain a reaction solution containing citalopram diol of formula 1;
and optionally
(5) post-treating the reaction solution containing citalopram diol obtained in step (4) to obtain a citalopram diol salt;
wherein, the reaction scheme is as follows:
wherein, X is Cl, Br or I.

5 more elements

Dependencies are inferred from the claim text.

Method for continuously preparing citalopram diol

Life of this patent

Method for continuously preparing citalopram diol

Life of this patent

Abstract

Claims20