FT-005, S-22954

Chemical Name: 2-(4,5-Dihydro-1H-imidazol-2-yl)-4-methyl-3,4-dihydro-2H-1,4-benzoxazine
CAS No. 96988-34-0, 97002-49-8 (diHCl)
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:The cyclization of 2-aminophenol (I) with ethyl 2,3-dibromopropionate (II) produced benzoxazine (III),which was converted to the corresponding formamide (IV) upon refluxing with formic acid.Reduction of (IV) with borane in THF gave rise to the N-methyl benzoxazine (V).Further treatment of (V) with ethanolic ammonia afforded amide (VI),which was dehydrated to nitrile (VII) by means of POCl3 in pyridine.Subsequent addition of MeOH to the nitrile group of (VII),followed by reaction with ethylenediamine yielded the target imidazoline.