Process for producing folic acid derivatives

Details Process for producing folic acid derivatives Process for producing folic acid derivatives

C - Chemistry, Metallurgy

07

F

C07F 7/10 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) C07B 53/00 (2006.01) C07D 475/04 (2006.01)

Patent

CA 2561374

An efficient process for producing a folic acid derivative being suitable for formation of a conjugate of anticancer drug and folic acid. There is disclosed a process comprising the step of conducting a reaction between a 2-amino protected pteroylimidazole and a .gamma.-lower alkyl glutamate to obtain a reaction product and the subsequent step of conducting a reaction between the reaction product and an amino compound having a reactive group capable of easily reacting with a functional group of drug.

Il est prévu un procédé efficace de fabrication d~un dérivé d~acide folique convenant à la formation d~un conjugué de médicament de lutte contre le cancer et d~un acide folique. Il est prévu un processus comprenant la phase de mise en réaction d~un ptéroylimidazole protégé 2-amino et d~un glutamate alkyle inférieur .gamma. pour obtenir un produit de réaction et la phase suivante de mise en réaction du produit de réaction et d~un composé amino ayant un groupe réactif capable de réagir facilement avec un groupe fonctionnel de médicament.

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