- Method for synthesizing gastric motility-promoting drug, i.e., domperidone
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The invention relates to a method for synthesizing a gastric motility-promoting drug, i.e., domperidone. The method comprises the following steps of adding 0.12mol of 5-chloro-1-(4-piperidyl)-benzimidazol-2-one (3), 1,100ml to 1,300ml of nitromethane, 0.31mol to 0.33mol of sodium sulfite, 0.13mol to 0.15mol of 1-(3-aminopropyl)benzimidazol-2-one and 3g to 5g of sodium bromide into a reaction vessel, carrying out refluxing for 30 hours to 32 hours while controlling the stirring rate to 110rpm to 130rpm, pouring the reaction solution into a sodium chloride solution, cooling the solution to the temperature of 3 DEG C to 5 DEG C so as to precipitate solids, washing the solids by a salt solution, carrying out washing by a toluene solution, carrying out dehydrating by a dehydrating agent, and carrying out recrystallization in propionitrile, thereby obtaining white solid domperidone, wherein the mass percent of the sodium chloride solution in the step is 15% to 20%, and the salt solution in the step is either a potassium sulfate solution or a sodium nitrate solution.
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Paragraph 0014; 0015
(2016/11/24)
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- 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds
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Compounds of the class of 1-(benzazolyalkyl)piperidine derivatives useful as antiemetic agents.
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