Process for preparation of indolopyrrolocarbazole...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/23 (2006.01) A61K 31/7056 (2006.01) A61P 35/00 (2006.01) C07C 241/02 (2006.01) C07C 243/14 (2006.01) C07H 19/044 (2006.01)

Patent

CA 2399209

This invention relates to a process for preparation of an indolopyrrolocarbazole derivative [I] by treating a compound[V] with a base in an inert solvent to prepare a compound [IV], reacting the obtained compound [IV] with a compound [III] to prepare a compound [II] and then removing the protective groups of the compound [II], the preparation intermediates compound [II], compound [III] and compound [IV], and processes for preparation of the compound [III]. (see formula V) (see formula IV) (see formula I) (see formula III) (see formula II) wherein Y1 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a phenyl group, a benzyloxymethyl group or an aralkyl group, R1, R2, R3, R4, R5 and R6 may be the same or different and each represent a protective group of a hydroxyl group, R7 and R8 may be the same or different and each represent a hydrogen atom or a protective group of a hydroxyl group, and X represents an acid molecule. This invention provides a safe and easy industrial preparation process of the indolopyrrolocarbazole derivative [I] useful as an antitumor agent.

L'invention concerne un procédé de préparation de dérivés d'indolopyrrolocarbazole (I) par traitement d'un composé (V) avec une base dans un solvant inerte afin de préparer un composé (IV), par réaction du composé (IV) avec un composé (III) afin de préparer un composé (II), et par déblocage du composé (II); des intermédiaires (II), (III) et (IV). L'invention concerne également un procédé de préparation des composés (III); Y<1> représente hydrogène, C1-4 alkyle, phényle, benzyloxyméthyle ou aralkyle; R<1>, R<2>, R<3>, R<4>, R<5> et R<6> représentent chacun individuellement un groupe protecteur hydroxyle; R<7> et R<8> représentent chacun individuellement hydrogène ou un groupe protecteur hydroxyle; X représentant une molécule d'acide. Il s'agit là d'un procédé industriel facile à réaliser et sûr, destiné à la préparation de dérivés d'indolopyrrolocabazole (1) utiles comme agents antitumoraux.

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