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    • 2. 发明专利
    • Method for producing phenoxy acetate derivative
    • 生产苯甲酸衍生物的方法
    • JP2012062263A
    • 2012-03-29
    • JP2010206453
    • 2010-09-15
    • Daiichi Sankyo Co Ltd第一三共株式会社
    • NAKAMURA YOSHITAKAUCHIDA KOSUKEOKABE TOSHIYUKI
    • C07C67/343C07B61/00C07C69/736
    • PROBLEM TO BE SOLVED: To provide a method for producing a phenoxy acetate derivative usable as an important synthetic intermediate in producing a medicine, etc.; and to provide the synthetic intermediate.SOLUTION: The method for producing a compound (I) being the phenoxy acetate derivative and represented by a general formula (I) (wherein Ris a 1-3C alkyl group; Ris a hydrogen atom, a 1-3C alkyl group, a 1-3C alkoxy group, or a fluorine atom; and Ris a 1-20C alkyl group or a 5-6C cycloalkyl group which may be optionally substituted) is characterized by adding and stirring hydrobromic acid and sodium nitrite into a compound (II) represented by a general formula (II) (wherein Rand Rare each described as above) in a solvent and then reacting the compound (II) with an acrylic ester (i) (wherein Ris described as above) in the presence of 4-hydroxy-2,2,6,6-tetramethyl piperidino-1-oxyl, 4-methoxyphenol and copper bromide.
    • 待解决的问题:提供一种制备可用作制备药物的重要合成中间体的苯氧基乙酸酯衍生物的方法等; 并提供合成中间体。 解决方案:制备由通式(I)表示的苯氧基乙酸酯衍生物的化合物(I)的方法(其中R 1 是1-3C烷基 基团; R 2 是氢原子,1-3C烷基,1-3C烷氧基或氟原子; R 其特征在于将氢溴酸和亚硝酸钠加入到通式(II)表示的化合物(II)中, (其中R 1 和R 2 各自如上所述)在溶剂中,然后使化合物(II)与 丙烯酸酯(i)(其中R如上所述描述)在4-羟基-2,2,6,6-四甲基哌啶子基-1-氧基,4 - 甲氧基苯酚和溴化铜。 版权所有(C)2012,JPO&INPIT
    • 3. 发明专利
    • Method for producing n-methylcarbamic ester derivative
    • 生产N-甲基胆碱衍生物的方法
    • JP2012062262A
    • 2012-03-29
    • JP2010206452
    • 2010-09-15
    • Daiichi Sankyo Co Ltd第一三共株式会社
    • NAKAMURA YOSHITAKAUMEO KAZUHIRO
    • C07C269/04C07B61/00C07C269/06C07C271/28
    • PROBLEM TO BE SOLVED: To provide a method for producing an N-methylcarbamic ester derivative capable of becoming an important synthetic intermediate in producing a medicine, etc.; and to provide the synthetic intermediate.SOLUTION: In the method for producing the N-methylcarbamic ester derivative being a compound (III) represented by a general formula (III), a compound (II) represented by a general formula (II) and obtained by reacting the amino group of a compound (I) represented by a general formula (I) with di-tert-butyldicarbonate in the presence of a base is reduced. In the general formula (I), Ris a 1-3C alkyl group; and R, Rand Rare the same or different and are each a hydrogen atom, a 1-3C alkyl group, a 1-3C alkoxy group, or a fluorine atom. In the general formula (II), R, R, Rand Rare the same as described above. In the general formula (III), Ris a 1-3C alkyl group; and R, Rand Rare the same or different and are each a hydrogen atom, a 1-3C alkyl group, a 1-3C alkoxy group, or a fluorine atom.
    • 待解决的问题:提供能够成为制备药物的重要合成中间体的N-甲基氨基甲酸酯衍生物的制造方法等; 并提供合成中间体。 解决方案:在由通式(III)表示的化合物(III)的N-甲基氨基甲酸酯衍生物的制造方法中,由通式(II)表示的化合物(II) 在碱存在下,由通式(I)表示的化合物(I)与二碳酸二叔丁酯组合。 在通式(I)中,R 1是C 1-3烷基; 和R 2 ,R 3 和R 4 是相同或不同的 各自为氢原子,1-3C烷基,1-3C烷氧基或氟原子。 在通式(II)中,R 1 ,R 2 ,R 3 < SP>和R 4 与上述相同。 在通式(III)中,R 1是C 1-3烷基; 和R 2 ,R 3 和R 4 是相同或不同的 各自为氢原子,1-3C烷基,1-3C烷氧基或氟原子。 版权所有(C)2012,JPO&INPIT