D83-7676

Chemical Name: 1-[2-Amino-6-[4-[3-[4-(3,5-difluorophenyl)piperazin-1-yl]-1(E)-propenyl]-5-methyl-1H-pyrazol-1-yl]pyrimidin-4-yl]azetidin-3-ol
CAS No. 256929-05-2 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Daiichi Pharmaceutical (Originator)
合成路线:The deprotection of the benzyloxypyrimidine derivative (I) by treatment wit TFA and thioanisole gives the hydroxypyrimidine (II),which is treated with hot POCl3,yielding the corresponding chloro derivative (III).Finally,the target compound is obtained by condensation of (III) with 3-hydroxyazetidine (IV) in refluxing ethanol.The azetidine (IV) is obtained by deprotection of 1-benzhydryl-3-hydroxyazetidine (V) by hydrogenation with H2 over Pd/C in ethanol/water.