Non-cross-linking pyrrolo(2,1-c)(1,4)benzodiazepines as...

Details Non-cross-linking pyrrolo(2,1-c)(1,4)benzodiazepines as... Non-cross-linking pyrrolo(2,1-c)(1,4)benzodiazepines as...

C - Chemistry, Metallurgy

07

D

C07D 519/00 (2006.01) A61K 31/5517 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2520898

The present invention relates to novel pyrrolo[2,1-c] [1,4]benzodiazepines compounds of general formula V as shown below, which are useful as potential antitumour agents and a process of preparing these compounds; particularly the present invention provides a process for the preparation of 7-methoxy-8-{n-[7- methoxy-(11aS)-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]ben-zodiazepine- 5-one-8-yloxy]alkyloxy}-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4] benzodiazepin-5-one, with varying aliphatic chain length and its 2-hydroxy derivatives. (F) wherein R and R1 is H and/or OH; and n is 3 to 5.

L'invention concerne des composés nouveaux de pyrrolo[2,1-c] [1,4]benzodiazépine ayant la formule générale V ci-dessous (dans laquelle R et R¿1? représentent H et/ou OH, et n est compris entre 3 et 5), qui sont potentiellement utiles comme agents anticancéreux, ainsi qu'un procédé de préparation de ces composés ; l'invention concerne notamment un procédé de préparation de 7-méthoxy-8-{n-[7-méthoxy-(11a<I>S</I>)-1,2,3,10,11,11a-hexahydro-5<I>H</I>-pyrrolo[2,1-c][1,4]benzodiazépin-5-one-8-yloxy]alkyloxy}-(11a<I>S</I>)-1,2,3,11a-tétrahydro-5<I>H</I>-pyrrolo[2,1-c][1,4]benzodiazépin-5-one avec une chaîne aliphatique de longueur variable, et de ses dérivés 2-hydroxyles.

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