Method for producing macrolide compound and production...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 407/06 (2006.01) C07D 295/18 (2006.01) C07F 7/22 (2006.01)

Patent

CA 2692644

The present invention provides a method for producing a 12-membered ring macrolide compound expected as a prophylactic or therapeutic agent for solid tumors and the like, and a production intermediate thereof. In detail, by acetalizing hydroxyl groups at 6- and 7-positions of a 12-membered ring macrolide compound being a raw material with dialkyl tin (IV) oxide and, after that, reacting the product with a carbamoyl halide derivative, the 7-position urethane derivative of the 12-membered ring macrolide compound being the target is effectively produced, without protecting hydroxyl groups at other positions.

L'invention porte sur un procédé de fabrication d'un composé macrolide ayant un cycle à 12 chaînons qui devrait être un agent préventif ou thérapeutique pour les tumeurs solides, etc. L'invention propose également un intermédiaire pour ce composé. Le procédé comporte l'acétalisation des groupes hydroxy dans les positions 6 et 7 d'un composé de départ macrolide ayant un cycle à 12 chaînons avec un oxyde de dialkyl étain (IV), puis la réaction du composé résultant avec un dérivé d'halogénure du carbamoyle. Ainsi, un dérivé d'uréthane en position 7 cible du composé macrolide ayant un cycle à 12 chaînons est obtenu avec un bon rendement sans la nécessité de protéger les groupes hydroxy dans les autres positions.

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