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INTERMEDIATE FOR SYNTHESIZING VINBLASTINE, METHOD FOR PRODUCING THE INTERMEDIATE, AND METHOD FOR SYNTHESIZING THE VINBLASTINE
INTERMEDIATE FOR SYNTHESIZING VINBLASTINE, METHOD FOR PRODUCING THE INTERMEDIATE, AND METHOD FOR SYNTHESIZING THE VINBLASTINE
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机译：合成长春花碱的中间体，制备中间体的方法和合成长春花碱的方法
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摘要
PROBLEM TO BE SOLVED: To provide a method for efficiently producing a natural-type vinbastine and analogues thereof, particularly, to provide intermediates useful for forming a carbomethoxyvelbanamine site, and to provide a method for efficiently producing the intermediate. SOLUTION: This intermediate of the general formula A (where, R1 , R2 , R3 and R4 are each a group selected independently from H, a lower alkyl, lower alkoxy, halogen atom, lower perfluoroalkyl, lower alkylthio, hydroxy, amino, mono- or dialkyl or acylamino, lower alkyl- or arylsulfonyloxy; R5 is H, a lower alkyl or substituted or nonsubstituted aryl; R6 is a =4C alkyl; R7 and R8 are each a substituted or nonsubstituted aryl; and R9 is an acryl or trialkylsilyl) useful for synthesizing a vinblastine. The 2nd objective method for producing the intermediate in high yield under mild conditions includes an indole synthesis method using thioanilide radical cyclization reaction and a 11-membered ring formation method using 2-nirobenzenesulfonamide intramolecular alkylation.
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机译：解决的问题：提供有效生产天然型长春花碱及其类似物的方法，特别是提供可用于形成碳氧甲氧基velbanamine位点的中间体，并提供有效生产该中间体的方法。溶液：通式A的中间体（其中R1，R2，R3和R4各自独立地选自H，低级烷基，低级烷氧基，卤素原子，低级全氟烷基，低级烷硫基，羟基，氨基，或二烷基或酰基氨基，低级烷基-或芳基磺酰氧基; R 5是H，低级烷基或取代或未取代的芳基; R 6是≤4C的烷基; R 7和R 8各自是取代或未取代的芳基;并且R 9是丙烯酸或三烷基甲硅烷基）对合成长春碱有用。在温和条件下高收率生产中间体的第二目的方法包括使用硫代苯胺基自由基环化反应的吲哚合成法和使用2-硝基苯磺酰胺分子内烷基化的11元环形成法。
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