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    • 8. 发明申请
    • PROCESS FOR THE PREPARATION OF INDOLE DERIVATIVES
    • 制备吲哚衍生物的方法
    • WO2003018555A1
    • 2003-03-06
    • PCT/EP2002/009046
    • 2002-08-13
    • CIBA SPECIALITY CHEMICALS HOLDING INC.WOLLEB, HeinzWOLLEB, AnnemarieVAN DER SCHAAF, Paul, AdriaanKOLLY, RomanEND, Nicole
    • WOLLEB, HeinzWOLLEB, AnnemarieVAN DER SCHAAF, Paul, AdriaanKOLLY, RomanEND, Nicole
    • C07D209/24
    • C07D405/06C07D209/24C07D319/06C07F5/025Y02P20/55
    • A process for the preparation of compounds of formula (I) wherein R 1 is unsubstituted or substituted C 1 -C 8 alkyl, R 2 , R 3 , R 4 and R 5 are each independently of the others hydrogen, unsubstituted or substituted C 1 -C 8 alkyl, C 1 -C 8 alkoxy, phenoxy or benzyloxy, or halogen, Y 1 and Y 2 are each independently of the other hydrogen or a protecting group, or Y 1 and Y 2 together form a protecting bridge, and X 1 is hydrogen, an organic radical or a cation, in which process a compound of formula (II) wherein R 1 R 2 R 3 , R 4 and R 5 are as defined above and Z 1 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 R 6 is hydrogen, bromine, chlorine, iodine, -OSO 2 CF 3 , -COCI, -B(OH) 2 or a mono- or di-ester derived from -B(OH) 2 , Y 3 and Y 4 are each a protecting group, or Y 3 and Y 4 together form a protecting bridge, and X 1 is as defined above, to form a compound of formula (IV) and if desired the radicals Y 3 and Y 4 are converted into the radicals Y 1 and Y 2 where Y 1 and Y 2 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为 转化为Y1和Y2基团,其中Y1和Y2是氢。