新产品编号:513077

Chemical Name: N-[2-(Dimethylamino)ethyl]-9-hydroxy-5,6,11-trimethyl-6H-pyrido[4,3-b]carbazole-1-carboxamide dihydrochloride
CAS No. 220443-16-3 (free base)
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:The title hemiglutarate ester was synthesized by acylation of the known olivacine derivative (I) with glutaric anhydride (II) in pyridine,followed by conversion to the corresponding dihydrochloride salt.

合成路线:The known pyridocarbazole (I) was methylated to (II) using dimethyl carbonate as the alkylating agent in the presence of K2CO3 and the phase-transfer catalyst adogen-464.For the preparation of the required amide (V),the ester group of (III) was first hydrolyzed with NaOH to the carboxylic acid (III),which was then coupled with 2-(dimethylamino)ethyl amine (IV) by means of (benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate (PyBOP) in hot N-methylpyrrolidone yielding (V).Finally,cleavage of the methyl ether of (V) with BBr3 provided the title compound.