Antitumour vinblastine and vincristine derivs. - e.g. 5'-nor-anhydro-vinblastine or vincristine, 5'-nor-leurosine and 12-chloro derivs. (J5 5.3.80)

• Main Author: NICOLE LANGLOIS, RATREMANIAINA ZO ANDRIAMIALISOA, YVES LANGLOIS ET PIERRE POTIER
• Format: Patent
• Language: English; French
• Published: 05.09.1980
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

(a) Vinblastine or vincristine derivs. of formula (I) and their acid addition and quat. ammonium salts and their acid addition and quat. ammonium salts and their 12-chloro derivs. are new. In (I), Qis a gp. (II) R'1 = H, alkoxy, acyl, formyl or haloacyl; R'2=H or alkyl; R'3,R"3 independently = H, hydroxy, alkanoyloxy or together = O or R'3 and R'5=-O- or form a second bond; R'4=H, alkoxycarbonyl, hydroxymethyl, alkanoyloxymethyl or acetamido; R'5, R"5 independently = H, hydroxy, alkanoyloxy, ethyl or 2-hydroxyethyl; R'6 = H, ethyl, 2-hydroxy-ethyl or acetyl. R1=H, alkyl, formyl or acyl; R2=H or alkoxy; R3=H hydroxy, or alkanoyloxy or R3 and R4 together = -O- or form a second bond; R4 = H, hydroxy, alkanoyloxy or R4 and R5 together = -O- R6 - alkoxycarbonyl, hydrazido, acetamido, hydroxymethyl or alkanoyloxymethyl; R5, R7=H, hydroxy or alkanoyloxy; R8 is H. (I) are antitumour agents which are prepd. administered parenterally esp. by i.v. injection in daily doses of 10-20 mg. for adults. LA PRESENTE INVENTION CONCERNE UN PROCEDE PERFECTIONNE DE PREPARATION DE DERIVES BIS-INDOLIQUES.IL S'AGIT D'UN PROCEDE DE PREPARATION DE COMPOSES SELON LA DEMANDE DE BREVET PRINCIPAL DANS LEQUEL ON TRAITE UN COMPOSE DE FORMULE:(CF DESSIN DANS BOPI)DANS LAQUELLE LES SUBSTITUANTS ONT LA SIGNIFICATION DONNEE AU BREVET PRINCIPAL ET X REPRESENTE UN HALOGENE, UN RADICAL HYDROXY, HYDROPEROXY OU ALCANOYLOXY.LES COMPOSES OBTENUS SONT UTILES COMME MEDICAMENTS.