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    • 71. 发明授权
    • Processes for preparing aminophenylsulfonylureas, and intermediates therefor
    • 制备氨基苯磺酰脲的方法及其中间体
    • US06500952B1
    • 2002-12-31
    • US09664201
    • 2000-09-18
    • Gerhard SchnabelJan VermehrenLothar Willms
    • Gerhard SchnabelJan VermehrenLothar Willms
    • C07D23942
    • C07D521/00A01N47/36H01R33/06Y02A40/143
    • The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, 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 (VIII) 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.
    • 本发明涉及化合物(Ⅰ)的制备,其中A = H或酰基,R 1,R 21,R 3,R 4,n,X,Y和Z如权利要求1中所定义,通过卤化和重排化合物 任选的盐),得到化合物(III)a)(III)至(IV)的氨解,硝基的还原和与式Ar-OCO-N(M)-Het的氨基甲酸酯(盐)(VI)的反应, 其中Ar =苯基,M = H或阳离子和Het =来自式(I)的杂环,得到(III)至(IV)化合物(I)(A = H),orb)氨解,与氨基甲酸酯 (VI)和还原所得化合物(VII)在NO 2基团上得到化合物(I)(A = H),orc)(III)与式HNR3-Het的氰酸酯和胺(VIII)的反应,还原 所得到的化合物(Ⅶ)在NO2基团上得到化合物(I)(A = H),任选的酰化如果A不为H.式(I)(A = H),(III) (IV),(V),(VI)(M =阳离子)和(VII)是新颖的。