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    • 7. 发明申请
    • Process for the preparation of indole derivatives
    • 吲哚衍生物的制备方法
    • US20050032875A1
    • 2005-02-10
    • US10487269
    • 2002-08-13
    • Heinz WollebAnnemarie WollebPaul Van Der SchaafRoman KollyNicole End
    • Heinz WollebAnnemarie WollebPaul Van Der SchaafRoman KollyNicole End
    • C07D209/12B01J31/18B01J31/24C07D209/24C07D319/06C07D405/06C07F5/02A61K31/405
    • C07D405/06C07D209/24C07D319/06C07F5/025Y02P20/55
    • A process for the preparation of compounds of formula (I) wherein R1 is unsubstituted or substituted C1-C8alkyl, R2, R3, R4 and R5 are each independently of the others hydrogen, unsubstituted or substituted C1-C8alkyl, C1-C8 alkoxy, phenoxy or benzyloxy, or halogen, Y1 and Y2 are each independently of the other hydrogen or a protecting group, or Y1 and Y2 together form a protecting bridge, and X1 is hydrogen, an organic radical or a cation, in which process a compound of formula (II) wherein R1 R2, R3, R4 and R5 are as defined above and Z1 is a leaving group, is reacted, in the presence of a catalytically effective amount of a palladium catalyst, with a compound of formula (III) wherein R6 is hydrogen, bromine, chlorine, iodine, —OSO2CF3, —COCI, —B(OH)2 or a mono- or di-ester derived from —B(OH)2, Y3 and Y4 are each a protecting group, or Y3 and Y4 together form a protecting bridge, and X1 is as defined above, to form a compound of formula (IV) and if desired the radicals Y3 and Y4 are converted into the radicals Y1 and Y2 where Y1 and Y2 are hydrogen.
    • 制备其中R 1为未取代或取代的C 1 -C 8烷基,R 2,R 3,R 4和R 5的式(I)化合物的方法各自独立地为氢,未取代或取代的C 1 -C 8烷基,C 1 -C 8烷氧基,苯氧基 或苄氧基或卤素,Y1和Y2各自独立地为另一个氢或保护基,或Y1和Y2一起形成保护桥,并且X 1是氢,有机基团或阳离子,其中式 (II)其中R1 R2,R3,R4和R5如上定义,Z1是离去基团,在催化有效量的钯催化剂存在下,与式(III)化合物反应,其中R 6是 氢,溴,氯,碘,-OSO 2 CF 3,-COCI,-B(OH)2或衍生自-B(OH)2,Y 3和Y 4的单酯或二酯各自为保护基,或Y 3和Y 4 一起形成保护桥,X1如上所定义,形成式(IV)的化合物,如果需要,基团Y 3和Y 4是 转化为Y1和Y2基团,其中Y1和Y2是氢。