C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) C07D 519/04 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2458600
Intermediates represented by the general formula (I) and being useful in the synthesis of vinblastines: [wherein R1, R2, R3, and R4 are each independently H, lower alkyl, lower alkoxy, halogeno, lower perfluoroalkyl, lower alkylthio, hydroxyl, amino, mono- or di-(alkyl or acyl)amino, or lower alkyl- or aryl- sulfonyloxy; R5 is H, lower alkyl, or substituted or unsubstituted aryl; R6 is alkyl having not more than four carbon atoms; R7 is substituted or unsubstituted aryl; R8 is substituted or unsubstituted aryl or lower alkyl; and R9 is acyl or trialkylsilyl]. A process for preparation of the above intermediates which comprises the synthesis of indole by radical cyclization of a thioanilide and the formation of a 11-membered cycle by intramolecular alkylation of 2-nitrobenzenesulfonamide and by which the reactions can proceed under mild conditions and high yield can be attained.
La présente invention concerne des intermédiaires représentés par la formule générale (I) et convenant à la synthèse des vinblastines. Dans cette formule R¿1?, R¿2?, R¿3?, et R¿4? sont chacun indépendamment H, alkyle inférieur, alcoxy inférieur, halogéno, perfluoroalkyle inférieur, alkylthio inférieur, hydroxyle, amino, mono- ou di-(alkyle ou acyle)amino, ou alkyle- ou aryle-sulfonyloxy inférieur; R¿5? est H, alkyle inférieur, ou aryle substitué ou non-substitué; R¿6? est C¿1?-C¿4? alkyle; R¿7? est aryle substitué ou non-substitué; R¿8? est aryle substitué ou non-substitué ou alkyle inférieur; enfin, R¿9? est acyle ou trialkylsilyle. L'invention concerne également l'obtention de ces intermédiaires par synthèse d'indole avec cyclisation des radicaux d'un thioanilide et formation d'un cycle à 11 segments par alkylation intramoléculaire de 2-nitrobenzène-sulfonamide, les réactions pouvant intervenir dans des conditions douces, avec un rendement élevé.
Fukuyama Tohru
Tokuyama Hidetoshi
Yokoshima Satoshi
Japan Science And Technology Agency
Smart & Biggar
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