867022-63-7Relevant academic research and scientific papers
A choline M receptor antagonists arab League bromine ammonium and its preparation method
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, (2016/12/22)
The invention relates to choline M receptor antagonist aclidinium bromide and a preparation method thereof. The chemical structural formula of the choline M receptor antagonist aclidinium bromide is as shown in the specification. The preparation method comprises the following steps: mixing R-quinine-3 alcohol, alkali and an organic solvent, dripping methyl oxalyl chloride, after the methyl oxalyl chloride is completely dripped, heating, performing heating reflux for 1-20 hours, and separating and purifying, thereby obtaining a substance A; adding iodine into a tetrahydrofuran solution of 2-bromothiophene and magnesium powder to initiate reaction for 1-5 hours, thereby preparing a Grignard reagent of 2-bromothiophene, adding the substance A, stirring to react for 10-30 minutes at the room temperature, performing heating reflux for 4-6 hours, separating and purifying, thereby preparing 2,2-dithienyl-2-glycolic acid-R-quinine-3-base ester, and performing quaterisation reaction with 3-phenoxypropyl bromine, thereby obtaining aclidinium bromide. The aclidinium bromide provided by the invention is simple in reaction operation, high in yield, low in price, short in reaction route, small in waste generation and easy in industrialization production.
