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    • 8. 发明申请
    • PROCESS FOR PREPARING N-ACETYLAMINOACETOPHENONES AND DOWNSTREAM PRODUCTS
    • 制备N-乙酰氨基戊二酸和下游产品的方法
    • WO2007039034A1
    • 2007-04-12
    • PCT/EP2006/008630
    • 2006-09-05
    • DSM FINE CHEMICALS AUSTRIA NFG GMBH & CO KGJARY, WaltherROGL, ChristianSKRANC, Wolfgang
    • JARY, WaltherROGL, ChristianSKRANC, Wolfgang
    • C07C231/10C07C233/07
    • C07C231/10C07C221/00C07C225/22C07C233/33
    • A process for preparing N-acetylaminoacetophenones of the formula (I) where R1 is a C 1 -C 8 -alkyl radical, C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, halocycloalkyl, formyl-C 1 -C 3 -alkyl or -C(=0)C(=0)R4, R2 is C 1 -C 4 -alkyl, C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, halocycloalkyl, formyl-C 1 -C 3 -alkyl, R3 is H, fluorine, chlorine, C 1 -C 4 -alkyl or trifluoromethyl and R4 is hydrogen, C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 3 -C 8 -cycloalkyl, wherein an indole of the formula (II) where R2 and R3 are as defined above and R5 is H or a C 1 -C 4 -alkyl radical, C 1 -C 8 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, C 1 -C 4 -alkoxy- C 1 -C 4 -alkyl, halocycloalkyl, formyl- C 1 -C 3 -alkyl, C(=0)C(=0)R4, where R4 is as defined above, is reacted with ozone in a suitable solvent from the group consisting of C 1 -C 6 -alcohols, nitriles, C 1 -C 4 -carboxylic acids or an anhydride thereof, C 1 -C 6 -alkyl acetates, chlorinated hydrocarbons, water and mixtures thereof and the peroxide solution obtained in this way is reduced and the desired N-acetylaminoacetophenone of the formula (I) is isolated, and also, if desired, conversion of the compound of the formula (I) into a compound of the formula (III) where R2 and R3 are as defined above.
    • 制备式(I)的N-乙酰基氨基苯乙酮的方法,其中R 1为C 1 -C 8 - 烷基,C 1〜 C 1 -C 6 - 烷基亚磺酰基,C 1 -C 6 - 烷基磺酰基,C 1 -C 4烷基亚磺酰基,C 1 -C 6 - / - 烷氧基-C 1 -C 4 - 烷基,卤代环烷基,甲酰基-C 1 -C 3 - 烷基或-C(= O)C(= O)R 4,R 2是C 1 -C 4 - 烷基,C 1〜 -C 6 - 烷基亚磺酰基,C 1 -C 6 - 烷基磺酰基,C 1 -C 4 烷氧基-C 1 -C 4 - 烷基,卤代环烷基,甲酰基-C 1 -C 3 - 亚烷基,R 3为H,氟,氯,C 1 -C 4 - 烷基或三氟甲基,R 4为氢,C 1〜 C 1 -C 8 - 烷基,C 1 -C 8 - 烷氧基,C 3 -C 8 其中式(II)的吲哚其中R 2和R 3如上定义,R 5是H或C 1 -C 4 - 烷基,C 1 -C 8 - 烷基亚磺酰基 C 1 -C 6 - 烷基磺酰基,C 1 -C 4 - 烷氧基-C 1 -C 6烷基磺酰基,C 1 -C 6 - C 1 -C 4烷基,卤代环烷基,甲酰基-C 1 -C 3 - 烷基,C(= O)C (= O)R 4,其中R 4如上定义,与臭氧在合适的溶剂中与C 1 -C 6 - 醇,腈, C 1 -C 4 -C 4 - 羧酸或其酸酐,C 1 -C 6 - C 6 - 烷基乙酸酯, 氯化烃,水及其混合物,并且以这种方式获得的过氧化物溶液被还原,并且分离所需的式(I)的N-乙酰基氨基苯乙酮,并且如果需要,将式(I)化合物转化为 其中R 2和R 3如上所定义的式(III)化合物。