CYPROHEPTADINE HYDROCHLORIDE synthesis

Yield:-

Reaction Conditions:

with hydrogenchloride in ethanol;water at 90; for 1 h;Large scale;

Steps:

1.4; 2.4; 3.4
4) Put a 16.4-kg crude 1-methyl 4- (5-hydroxy-5-dibenzo [a, e] cycloheptatrienyl) piperidine in a 2000 mL round bottom bottle,Add 38L of 95% by mass ethanol aqueous solution to heat and dissolve, and then add 1.2L of 35% by mass concentrated hydrochloric acid.Continue to heat to 90 ° C and stir the reaction for 1h, cool slightly, add 180g of activated carbon, heat and stir for 20min, filter while hot, wash the filter residue with a small amount of hot water, and combine the filtrates to stand for crystallization at room temperature.Filtration and drying at 80-100 ° C gave 12.7 kg of cyproheptadine hydrochloride as a white crystalline powder with a purity of 93.3% and a yield of 74.2%. Further,The obtained cyproheptadine hydrochloride was dissolved in a 20% ethanol aqueous solution and recrystallized to obtain a purified cyproheptadine hydrochloride with a purity of 99.9% and a yield of 68%.

References:

Guangzhou Puxing Pharmaceutical Co., Ltd.;Pu Hanlin;Zheng Zhongwang;Zhu Yibo;Xiang Dongfang CN110407737, 2019, A Location in patent:Paragraph 0049; 0054; 0056; 0061; 0063; 0068; 0070; 0075

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