144025-04-7Relevant articles and documents
Chiral c-KIT inhibitor drug key intermediate and preparation method thereof
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Paragraph 0138; 0140; 0143; 0144, (2020/07/24)
The invention relates to a preparation method of a c-KIT inhibitor shown in a formula (III), key intermediates shown in a formula (I) and a formula (II) and a preparation method of the intermediates,and definitions of substituent groups in the formula (I)
Synthetic method for antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane
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Paragraph 0043; 0049; 0055; 0061; 0067, (2016/10/07)
The invention discloses a synthetic method for an antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane. The synthetic method comprises the following steps: (1) reacting a compound IV with a Grignard reagent to obtain a compound III; (2) employing a one-pot reaction to react the compound III with trimethylsulfoxonium iodide and 1,2,4-triazole and then react with p-toluenesulfonic acid, so as to obtain a compound II; and (3) reacting the compound II with methanesulfonyl chloride under an alkali condition to generate the target compound I, wherein the Grignard reagent is 2,4-difluorophenylmagnesium bromide or 2,5-difluorophenylmagnesium bromide, and the structural formula of the compound IV is shown in the specification. According to the synthetic route, the reaction conditions are mild and easy to control, the reaction route is simple, the related solvents in the reaction process all are common solvents, the reaction conversion rate is high, and the method possesses extremely high feasibility, is beneficial for industrialized batch production, and possesses extremely large exploitation potential and extremely good application prospect.
ANTIFUNGAL COMPOUND PROCESS
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Page/Page column 89, (2015/11/10)
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.