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    • 8. 发明申请
    • Process for Producing Thiazolidinedione Compound and Production Intermediate Thereof
    • 生产噻唑烷二酮化合物及其制备方法
    • US20080103185A1
    • 2008-05-01
    • US11795270
    • 2006-01-24
    • Yoshitaka NakamuraChiharu SatohHiroshi MiyamotoHisaki Kajino
    • Yoshitaka NakamuraChiharu SatohHiroshi MiyamotoHisaki Kajino
    • A61K31/427A61P3/00A61P3/06A61P3/10A61P9/10C07D417/12
    • C07D417/12C07D277/34Y02P20/55
    • There are provided crystals of a thiazolidinedione derivative having excellent prophylactic and therapeutic effects on a disease caused by insulin resistance and a process for producing the thiazolidinedione derivative with a high purity. As described above, a process for producing a compound represented by the general formula (A) or a salt thereof, comprising converting 4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetic acid represented by the following formula into a compound of the general formula (I), wherein X=a halogen atom; then reacting the compound with a compound represented by the general formula (II), wherein R1, R2, R3 and R4=a hydrogen atom, a hydroxyl group, C1-C6 alkyl, C1-C6 alkoxy, benzyloxy, acetoxy, trifluoromethyl or a halogen atom, R5=C1-C6 alkyl, and R6=a protecting group for an amino group, to produce a compound represented by the general formula (III); and subsequently cyclizing the compound into the final product, and crystals of a compound represented by the general formula (A) or a salt thereof.
    • 提供了对由胰岛素抵抗引起的疾病具有优异的预防和治疗效果的噻唑烷二酮衍生物的晶体和具有高纯度的噻唑烷二酮衍生物的制备方法。 如上所述,制备由通式(A)表示的化合物或其盐的方法,包括将由下式表示的4 - [(2,4-二氧代噻唑烷-5-基)甲基]苯氧基乙酸转化为 通式(I)的化合物,其中X =卤素原子; 然后使化合物与通式(II)表示的化合物反应,其中R 1,R 2,R 3和R SUP > 4 =氢原子,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,苄氧基,乙酰氧基,三氟甲基或卤素原子,R 5 = C 1 -C 6烷基, 和R 6 =氨基的保护基,以制备由通式(III)表示的化合物。 随后将化合物环化成最终产物,和由通式(A)表示的化合物或其盐的晶体。