新产品编号:1536631

Chemical Name: 2-Amino-N-[2-[2-fluoro-4-(methylamino)phenyl]-1-methylethyl]acetamide acetate
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:Reaction of 3-fluoroaniline (I) with formic acid gave formanilide (II),which was reduced by means of LiAlH4 to afford 3-fluoro-N-methylaniline (III).Further alkylation of (III) with benzyl chloride provided the tertiary amine (IV).Vilsmeier-Haack formylation of (IV) with POCl3 and DMF yielded aldehyde (V),which was condensed with nitroethane in the presence of ammonium acetate to give the 2-nitropropene derivative (VI).After reduction of (VI) to the amine (VII) with LiAlH4,condensation with chloroacetyl chloride afforded chloracetamide (VIII).Subsequent displacement of the chlorine of (VIII) with dibenzylamine yielded the tertiary amine (IX).Finally,hydrogenolytic debenzylation of (IX) in the presence of Pd/C furnished the title compound.