SYNTHESIS METHOD FOR CANDESARTAN CILEXETIL INTERMEDIATE

    公开(公告)号:EP3907215A1

    公开(公告)日:2021-11-10

    申请号:EP19908010.2

    申请日:2019-01-02

    Abstract: A synthesis method for a candesartan cilexetil intermediate represented by formula (II). The method comprises: (1) dissolving a compound represented by formula (IV) to an aprotic solvent to obtain a first mixed solution, and dissolving a phase transfer catalyst and an azidation reagent to water to obtain a second mixed solution; (2) dropping the first mixed solution to the second mixed solution for azidation reaction, and after the reaction is ended, standing and layering same to obtain an organic phase containing a compound represented by formula (V); (3) dropping the obtained organic phase containing the compound represented by formula (V) to tertiary butyl alcohol for rearrangement reaction, and after the reaction is ended, concentrating same to obtain a solid or oily material, then adding a crystallizing solvent to the obtained solid or oily material for recrystallization, and separating same to obtain a crystal, i.e., the candesartan cilexetil intermediate represented by formula (II). The synthesis method of the present application does not require the use of a DMF solvent, is safe and environmentally friendly, and reduces generation of ammonia nitrogen wastewater.

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