Lerner, David, Littenberg, Krumholz & Mentlik, LLP
Intermediate and process of preparation of ecteinascidin such as ecteinascidines-583,597 using such intermediate
The present invention concerns an intermediate of the following formula (I) in which R1 and R2 represent independently of each other a C1-C12 alkyl group, a (C1-C12 alkoxy)carbonyl group, optionally substituted by one, two or three halogen atom, a (C2-C12 alkenyloxy)carbonyl group, an acyl group, a aryl(C1-C12)alkyl group, an arylalkoxy carbonyl group, a (C1-C12 alkyl)sulfonyl group or an arylsulfonyl group, R3 represents a O-protecting group, R4 and R5 represent independently of each other a hydrogen atom or a O-protecting group, R6 represent a O-protecting group and R7 represent a C1-C12 alkyl group or —OR6 and —OR7 form together a group —OCH2O—. The present invention concerns also a process of preparation of the intermediate and its use for the preparation of Ecteinascidin 743 and Ecteinascidin-770.
Centre National de la Recherche Scientifique (CNRS)
C Y
C07D Y02P
inventional additional
Jinchun Jieping Michèle Xiaochuan
Chen Zhu Bois-Choussy Chen