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    • 1. 发明授权
    • Processes for the preparation of aminophenylsulfonyl-ureas and intermediate products for the processes
    • 用于制备氨基苯磺酰脲和中间产物的方法
    • US06790955B2
    • 2004-09-14
    • US10288052
    • 2002-11-05
    • Gerhard SchnabelJan VermehrenLothar Willms
    • Gerhard SchnabelJan VermehrenLothar Willms
    • C07D27300
    • C07D521/00A01N47/36H01R33/06Y02A40/143
    • The invention relates to the preparation of compounds (I) in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A═H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.
    • 本发明涉及其中A = H或酰基和R 1,R 2,R 3,R 3,n,X,Y和Z如权利要求1中所定义的化合物(I)的制备, 化合物(II)(任选盐)的卤化和重排以得到化合物(III)a)(III)至(IV)的氨解,还原硝基并与式Ar-的氨基甲酸酯(盐)(Ⅵ) 其中Ar =苯基,M = H或阳离子和Het =来自式(I)的杂环,得到化合物(I)(A = H),orb)氨解(III)至(III) IV),与氨基甲酸酯(盐)(VI)的反应和NO 2基团上得到的化合物(VII)的还原,得到化合物(I)(A = H),orc)(III)与氰酸酯和胺的反应(VII) 的式(HNR 3)-Het,并且在NO 2基上还原所得化合物(Ⅶ),得到化合物(I)(A = H),并且如果A不为H,则为任意的酰化。式 I)(A = H),(III),(IV),(V),(VI)(M =阳离子)和(VII)