新产品编号:2392493

Chemical Name: N5-(2-Chlorobenzyl)-N5-methyl-6-[6-(4-morpholinyl)pyridin-3-ylethynyl]pyrimidine-4,5-diamine
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Reaction of 2,5-dibromopyridine (I) with morpholine (II) yields 5-bromo-2-(4-morpholinyl)pyridine (III).Palladium-catalyzed coupling of (III) with trimethylsilyl acetylene (IV) leads to the ethynylpyridine (V)

合成路线:Iodination of 5-amino-4,6-dichloropyrimidine (VI) by means of NaI in concentrated HI affords the diiodopyridine (VII).Sequential alkylation of aminopyrimidine (VII) with 2-chlorobenzyl bromide (VIII) to produce (IX),and further N-methylation with iodomethane and NaH,lead to the tertiary amine (X).Ammonolysis of the diiodopyrimidine (X) with ethanolic ammonia in a sealed tube at 80 C yields amine (XI).Finally,Sonogashira coupling between acetylene (V) and iodopyrimidine (XI) in the presence of Pd(PPh3)2Cl2 and CuI furnishes the target diaryl acetylene