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ChemicalBook CAS DataBase List Lomerizine hydrochloride

Lomerizine hydrochloride synthesis

3synthesis methods
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Yield: 87.4%

Reaction Conditions:

Stage #1:4,4'-difluorobenzhydryl chloride;1-(2,3,4-trimethoxybenzyl)piperazine with triethylamine in methanol at 65 - 75; for 10 h;
Stage #2: with hydrogenchloride in ethanol at 45; for 2 h;

Steps:

1; 3
1-(2,3,4-Trimethoxybenzyl)piperazine (24.0 g, 0.09 mol) was dissolved in 200 mL of methanol then 4,4'-difluorodiphenylmethyl chloride (21.5 g, 0.09 mol) ) and triethylamine (18.2g, 0.18mol), under the condition of 65 °C ~ 75 °C tirred 10H, then cooled to 40 °C ~ 50 °C, temperature 40 °C ~ 50 °C fractions were concentrated under reduced pressure to not give 1- (R-(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine crude.

References:

Chenxin Pharmaceutical Co., Ltd.;Zhang Lebo;Sun Shoufei;Zhang Baikun;Li Zhongjing;Jiang Ruiling CN109666008, 2019, A Location in patent:Paragraph 0016; 0018; 0022; 0024; 0030; 0031

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