137887-27-5Relevant articles and documents
Method for synthesizing ramosetron hydrochloride through ramosetron
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Paragraph 0031; 0032; 0053, (2016/10/31)
The invention discloses a method for synthesizing ramosetron hydrochloride through ramosetron, and belongs to the technical field of organic synthesis. According to the method, on the basis of the prior art, the technological conditions for synthesizing ramosetron hydrochloride through ramosetron are optimized; the method comprises the steps that butyl acetate is added to ethyl alcohol and ramosetron, an ethanol hydrochloride solution is dropwise added to adjust the pH to be 1.5-2 on the condition that the temperature ranges from 30 DEG C to 35 DEG C, acetonitrile is added, and the temperature is decreased to 0-2 DEG C; pyrrolidine is dropwise added, the temperature is increased to room temperature, a reaction is conducted for 0.5 h, and pressure reduction is conducted to remove acetonitrile; a saturated sodium chloride solution is added, chloroform extraction is conducted, and organic phases are mixed; metal rhodium is added, stirring is conducted for 1-1.5 h, filtering is conducted, a filter cake is leached with a small amount of ethanol and then directly treated with 0-5 DEG C ethanol, standing is conducted all night, recrystallization is conducted, and ramosetron hydrochloride is obtained. By means of the method, the yield of ramosetron hydrochloride is increased, the reaction safety is improved, the reaction time is shortened, and the higher economic benefit is achieved.