Preparation Method For Losartan
    1.
    发明申请

    公开(公告)号:US20220388988A1

    公开(公告)日:2022-12-08

    申请号:US17629990

    申请日:2020-01-17

    IPC分类号: C07D403/10

    摘要: Provided is a preparation method of losartan, which is prepared by reacting a cyano group-containing intermediate represented by formula (I) with an azide reagent in toluene in the presence of a catalyst; wherein, after the reaction is completed, azide ions are removed by means of the following process: adding water to divide the reaction system into three layers, separating the intermediate layer and adding n-butanol to the intermediate layer for dilution, and adding triphenylphosphine to the resulting diluted solution so as to remove residual azide ions from the diluted solution. The preparation method provided by the present invention does not need to use sodium nitrite, thus fundamentally eliminating the formation of genotoxic impurities nitrosamines. The resulting target product has good purity, high yield, a simple preparation process, mild and easy-to-control operating conditions, and good safety, and is suitable for large-scale industrial production,

    Method for preparing anti-heart-failure medicine LCZ696

    公开(公告)号:US10221145B2

    公开(公告)日:2019-03-05

    申请号:US16060297

    申请日:2016-06-06

    IPC分类号: C07D257/02 B01D9/00 A61P9/12

    摘要: The present invention discloses a method for preparing an anti-heart-failure medicine LCZ696. The preparing method comprises the following step (formula (I)): in an organic solvent, a Sacubitril dicyclohexylamine salt reacts with valsartan under the effect of a sodium hydroxide aqueous solution, and the anti-heart-failure medicine LCZ696 is obtained. The preparing method of the present invention is simple in process and omits the procedures of ion exchange from a sodium salt to a calcium salt and hydrochloric acid dissociation in an existing production process, residues of calcium ions are avoided, and the production efficiency is effectively improved.