Patent ID: 7420052

Claim:
A method for synthesis of (+)-vinblastines represented by formula F wherein R 1 , R 2 , R 3 and R 4 are 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, R 5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R 6 is an alkyl group of carbon number 4 or less, R 14 , R 15 and R 16 are an alkyl group of carbon number 4 or less, R 17 is H or an alkyl group of carbon number 4 or less, and in between carbon 14 and carbon 15 is an unsaturated double bond or saturated bond, comprising, chlorination of 3 site of indole by treating indole derivatives of formula A with t-butylhypochlorite, wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 have the same meaning as in formula F, R 7 is a substituted or non-substituted aryl group, R 8 is a substituted or non-substituted aryl group or lower alkyl group and R 9 is an acyl group or trialkylsilyl group, preparing the compound of formula E by coupling of vindolines by the treatment of the obtained chlorinated product with trifluoroacetic acid under the presence of vindolines, then removing trifluoroacetyl group and SO 2 R 7 , and forming a piperidine ring, wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , have same meaning to the case of formula F; R 7 , R 8 , and R 9 , have same meaning to the case of formula A; and R 14 , R 15 , R 16 , and R 17 have same meaning to the case of formula F, and in between carbon 14-carbon 15 is an unsaturated double bond or saturated bond.