76159-92-7Relevant articles and documents
Synthesis technology of cardiovascular medicine Apabetalone
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Paragraph 0032; 0037; 0040; 0041; 0050; 0059, (2019/01/08)
The invention discloses a synthesis technology of a cardiovascular medicine Apabetalone, and relates to the technical field of organic synthesis of medicines. The synthesis technology comprises the following steps: with 3,5-dimethoxyaniline as a raw material, firstly performing a condensation reaction on the 3,5-dimethoxyaniline, hydroxylamine sulfate and chloral hydrate to obtain N-(2,4-dimethoxyphenyl)-2-(oximido)acetamide, then performing a cyclization reaction to obtain 5,6-dimethoxy isatin under the effect of concentrated sulfuric acid, then performing an oxidation reaction on the 5,6-dimethoxy isatin and ammonia water or ammonia gas to obtain 2-amino-4,6-dimethoxybenzonitrile in the presence of divalent copper and an oxidant, finally performing a condensation reaction on the 2-amino-4,6-dimethoxybenzonitrile and 4-(2-hydroxyethoxy)-3,5-dimethylbenzaldehyde in an organic solvent under the effect of an alkaline substance to obtain the Apabetalone. Compared with the synthesis technology recorded in the existing literature, the synthesis technology provided by the invention has the advantages as follows: the raw material is cheap and easy to obtain, a reaction condition is mild,high-temperature and high-pressure conditions are not required, the posttreatment operation is simple, a synthesis route is short, and industrial production is easy.
