UR-1827

Chemical Name: 2-(1-Benzylpiperidin-4-yl)-1-[4-(5-methylpyrimidin-4-ylamino)phenyl]-1-ethanone
CAS No. 158973-91-2
项目整合开发状态: Preclinical
项目研究机构: Ube (Originator)
合成路线:The condensation of 1-benzylpiperidin-4-one (I) with 4-acetamidoacetophenone (II) by means of lithium diisopropylamide in HMPA/THF gives the piperidinol (III),which is dehydrated by reaction first with SOCl2 and then with NaOH yielding a mixture of compounds (IV) and (V) with exo and endo double bonds.This mixture is hydrogenated with H2 over PtO2 in ethanol/toluene to afford the saturated piperidine derivative (VI),which is treated with HCl in refluxing ethanol to cleave the acetamido substituent giving (VII) with a free amino group.Finally,this compound is condensed with 4-chloro-5-methylpyrimidine (VIII) by means of HCl in refluxing ethanol/CHCl3.