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ChemicalBook CAS DataBase List Trimetazidine

Trimetazidine synthesis

3synthesis methods
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Yield:5011-34-7 92.1%

Reaction Conditions:

Stage #1:2,3,4-trimethoxybenzyl chloride;1-t-Butoxycarbonylpiperazine with methanol;sodium hydroxide at 35 - 45; for 4 h;
Stage #2: with hydrogenchloride in water at 35 - 45; for 2 h;

Steps:

1 Preparation of 1-(2,3,4-trimethoxybenzyl)piperazine
2,3,4-Trimethoxybenzyl chloride (21.7 g, 0.1 mol) was dissolved in 200 mL of methanol, then 1-Boc-piperazine (22.4 g, 0.12 mol) and 2 mol/L sodium hydroxide solution 25 ml were added. Stir at 35 °C ~ 45 °C for 4 h, thenadd 100 ml of 1 mol / L hydrochloric acid solution, stir at 35 °C ~ 45 °C for 2 h, then concentrate the methanol under reduced pressure, then add 100 ml ofpurified water, with 1 mol / The sodium hydroxide solution of L was adjusted to pH 7-8, and the solid was precipitated. The solid was suction filtered, and the filter cake wasrinsed twicewith 50 ml of purified water, and then the filter cake was dried in a blast oven at 50 °C for 8 to 10 hours. 24.5 g of the target product 1-(2,3,4-trimethoxybenzyl)piperazine was obtained in a yield of 92.1%.

References:

Chenxin Pharmaceutical Co., Ltd.;Zhang Lebo;Sun Shoufei;Zhang Baikun;Li Zhongjing;Jiang Ruiling CN109666008, 2019, A Location in patent:Paragraph 0016; 0018; 0019; 0020; 0021

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