Intermediates for synthesis of vinblastine, process for...

Details Intermediates for synthesis of vinblastine, process for... Intermediates for synthesis of vinblastine, process for...

2006-08-15

2008-09-02

Coleman, Brenda L (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

Reexamination Certificate

active

07420052

ABSTRACT:
An intermediate for vinblastine synthesis represented by general formula A.general formula A.(in the formula, R1, R2, R3and R4are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6is an alkyl group of carbon number 4 or less, R7is a substituted or non-substituted aryl group, R8is a substituted or non-substituted aryl group or lower alkyl group and R9is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.

REFERENCES:
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