IP Library › Granted Patent US 12668566
Granted Patent B2
US 12668566 · App. 17/613,834 · Granted Jun 30, 2026

Preparation method for salicylamine acetate

Inventors: Ling Long (Shanghai, CN); Jianyi Ma (Shanghai, CN); Weiguo Liu (Shanghai, CN); Zhouya Liu (Shanghai, CN)
Assignee: TSI Group Co., Ltd.
C07C213/02C07C51/412
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Quick Facts
Patent No.
US 12668566
App. No.
17/613,834
Granted
Jun 30, 2026
Kind
B2
Abstract

A preparation method for salicylamine acetate, comprising preparing an amino-protected intermediate from salicylaldehyde, and reacting the intermediate with acetic acid to prepare an acetate.

Claims (15)

1 . A method for preparing salicylamine acetate, wherein the method comprises the following steps:

(1) subjecting salicylaldehyde having a structure shown in Formula 1

to amino protection to obtain a compound having a structure shown in Formula 2

(2) reacting the compound having the structure shown in Formula 2 with acetic acid to obtain salicylamine acetate in one step, wherein the ratio of the compound of Formula 2 to acetic acid in step (2) is 1:1-20 (g/ml) and the temperature for reacting with acetic acid in step (2) is from 70° C. to the reflux temperature of acetic acid.

2 . The method according to claim 1 , wherein the reaction temperature of amino protection in step (1) is 0-50° C.

3 . The method according to claim 1 , wherein the reaction time of amino protection in step (1) is 3-18 hours.

4 . The method according to claim 1 , wherein the reaction solvent in step (1) is selected from the group consisting of tetrahydrofuran, 2-methyltetrahydrofuran, acetonitrile and 1,4-dioxane.

5 . The method according to claim 1 , wherein the ratio of the compound of Formula 2 to acetic acid in step (2) is 1:1-15 (g/mL).

6 . The method according to claim 1 , wherein the ratio of the compound of Formula 2 to acetic acid in step (2) is 1:3-10 (g/mL).

7 . The method according to claim 1 , wherein the method comprises the following steps:

(1) protecting the salicylaldehyde having the structure shown in Formula 1 with an amino group to obtain the compound having the structure shown in Formula 2;

(2) reacting the compound having the structure shown in Formula 2 with acetic acid, and lowering the temperature to room temperature after the reaction is complete, to obtain crude salicylamine acetate;

(3) mixing the obtained crude salicylamine acetate with an organic solvent and crystallizing to obtain pure salicylamine acetate; wherein the organic solvent is selected from the group consisting of ethyl acetate, isopropyl ether, absolute ethanol and methyl tert-butyl ether.

8 . The method according to claim 1 , wherein the time for reacting with acetic acid in step (2) is 5-70 hours.

9 . The method according to claim 1 , wherein the time for reacting with acetic acid in step (2) is 5-60 hours.