752174-62-2Relevant articles and documents
Preparation method and application of sacubitril intermediate
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Paragraph 0059-0062, (2021/07/17)
The invention discloses a preparation method and application of a sacubitril intermediate. The sacubitril intermediate disclosed by the invention is obtained by taking itaconic anhydride as a raw material, performing chiral reduction, esterification, selective hydrolysis and carboxyl activation, and finally conducting coupling with 4-biphenylacetic acid. The invention also provides a method for preparing sacubitril by using the sacubitril intermediate. The preparation method provided by the invention has the advantages of easily available raw materials, simple process, economy, environmental protection and the like, and is more suitable for industrial production compared with other routes.
SACUBITRIL INTERMEDIATE AND PREPARATION METHOD THEREOF
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, (2019/01/04)
The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril. The method disclosed herein has advantages of easily obtained raw materials, simple preparation process, low cost, environment friendly, and etc., which is very suitable for industrial production.
Method for preparing LCZ696 impurity reference substance
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Paragraph 0026; 0027; 0028; 0041; 0042; 0043; 0044-0049, (2017/11/30)
The invention provides a method for preparing an LCZ696 impurity reference substance. The method comprises the following steps: performing a reaction on (2R, 4S)-5-(biphenyl-4-yl)-4-[(t-butyloxycarboryl) amino]-2-methylpentanoic acid and thionyl chloride in ethanol so as to obtain a compound of formula I; performing a reaction on the compound of the formula I under a weak alkali condition so as to obtain a compound of formula II; performing heating reflux on succinic anhydride in isopropanol so as to obtain a compound of formula III; performing a reaction on the compound of the formula III with thionyl chloride so as to obtain a compound of formula IV; preparing the LCZ696 impurity reference substance of formula V from the compound of the formula II and the compound of the formula IV under catalysis of a strong alkali catalyst. By adopting the method provided by the invention, consumption of raw materials is reduced as a whole, the method is economic and environmental-friendly, different steps of reactions can be relatively easily implemented and controlled, meanwhile the amount of heavy metal catalysts is reduced and avoided, and the quality indexes of final products are improved.