1073553-77-1Relevant articles and documents
Aliskiren intermediate preparation method
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Paragraph 0091; 0095; 0096, (2019/03/25)
The present invention relates to the technical field of pharmaceutical preparation method, the preparation method of the existing long reaction time, the problem of low yield, provides a aliskiren preparation method, comprises the following steps: S1, 1st intermediate preparation: the raw material is dissolved in a solvent, adding sodium hypochlorite and sodium bisulfite reaction, shall be 1st intermediate; S2, intermediate in the preparation of 2nd: to the 1st intermediate dropping 4 - bromo - 1 - methoxy - 2 - (3 - methoxy third oxygen radical) benzene, tetrahydrofuran solution, adding low [...] catalyst, to obtain the 2nd intermediate; S3, aliskiren intermediate preparation: will be soluble in ethyl acetate in the 2nd intermediate, then adding water, nitrogen replacement 3 times, the hydrogen replaced 3 times after adding the hydrogen hydrogenation reaction, to obtain the product. By adding low deuterium water as a catalyst, help to accelerate the step S2 of the reaction rate, the reaction time is shortened, while at the same time help to improve the step S2 in the reaction yield, and then make the total reaction yield can be improved.