Histaprodifen

Chemical Name: 2-[2-(3,3-Diphenylpropyl)-1H-imidazol-4-yl]-1-ethanamine
项目整合开发状态: Preclinical
项目研究机构: Freie Universit鋞 Berlin (Originator)
合成路线:3,3-Diphenylpropionic acid (I) was treated with SOCl2 to give acid chloride (II) and then converted to amide (III) using liquid ammonia.Dehydration with P2O5 led to diphenylpropionitrile (IV),which was treated with SOCl2 in methanol to afford the iminoester (V).The condensation of (V) wiith 2-oxobutan-1,4-diol (VI) in liquid ammonia furnished imidazole (VII).Further treatment of (VII) with SOCl2 provided chloride (VIII).Finally,reaction of (VIII) with methylamine in the presence of K2CO3 and a catalytic amount of KI afforded the title compound.

合成路线:3,3-Diphenylpropionic acid (I) was treated with SOCl2 to give acid chloride (II) and then converted to amide (III) using liquid ammonia.Dehydration of (III) with P2O5 led to diphenylpropionitrile (IV),which was treated with ammonia in methanol to afford the iminoester (V).The condensation of (V) with 2-oxo-4-phthalimido-1-butyl acetate (VI) in liquid ammonia furnished imidazole (VII).Finally,deprotection of the phthaloyl group of (VII) with methanolic hydrazine afforded the title compound.">