Solid phase synthesis of antitumoral compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 491/14 (2006.01) C07D 207/34 (2006.01)

Patent

CA 2515313

Lamellarins are prepared using a solid phase synthesis. In a first aspect, the process includes a step as follows: Formula (I) where R1 to R15 are as defined, and X is halogen, provided that one of R2, R3 or R4 is immobilised to a resin. In a second aspect, the process includes a step as follows: Formula (II) where R1' to R5', R11' and R13' are as defined, X1 and X2 are halogen, M is a metal function and PG is an amino protecting group, provided that one of that R2', R3' or R4' is immobilised to a resin.

On prépare des Lamellarines en utilisant une synthèse en phase solide. Dans un premier aspect, le processus comprend ce qui suit: formule (I) dans laquelle R¿1? à R¿15? sont définis dans la description, et X est un halogène, à condition que un des R¿2?, R¿3? ou R¿4 est ?soit immobilisé sur une résine. Dans un second aspect, le processus comprend ce qui suit: formule (II) dans laquelle R¿1?' à R¿5?', R¿11?' et R¿13?' sont définis dans la description, X¿1? et X¿2 ?sont des halogènes, M est une fonction métallique et PG est groupe amino protecteur, à condition que un des R¿2?', R¿3?' or R¿4?' soit immobilisé sur une résine.

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