RS-127445

2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐 Chemical Name: 4-(4-Fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine
CAS No. 199864-87-4, 199864-86-3 (mono HCl salt)
项目整合开发状态: Phase I
项目研究机构: Roche Bioscience (Originator)
合成路线:Cyclization of ethyl 4-methyl-3-oxopentanoate (I) with guanidine carbonate (II) in boiling EtOH gave 2-amino-4-hydroxy-6-isopropylpyrimidine (III),which was converted to the corresponding chloropyrimidine (IV) by means of POCl3.Boronic ester (VI) was prepared by lithiation of 1-bromo-4-fluoronaphthalene (V) with n-butyllithium,followed by reaction with trimethyl borate.Subsequent coupling of chloropyrimidine (IV) with boronic ester (VI) in the presence of tetrakis(triphenylphosphine)palladium yielded the target naphthylpyrimidine.