FR-177995

Chemical Name: 2,6-Dichloro-N-[1-[2-(4-morpholinyl)-2-oxoethyl]-2-(trifluoromethyl)-1H-benzimidazol-4-yl]benzamide
CAS No. 189043-21-8
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:Condensation of 3-nitro-1,2-phenylenediamine (I) with trifluoroacetic acid provided benzimidazole (II).Reduction of the nitro group of (II) by means of hydrazine in the presence of FeCl3 and activated carbon gave amine (III),which was coupled with 2,6-dichlorobenzoyl chloride (IV) yielding amide (V).Alkylation of (V) with tert-butyl bromoacetate afforded benzimidazoleacetic acid tert-butyl ester (VI).After trifluoroacetic acid-promoted cleavage of the tert-butyl ester of (VI) the resulting carboxylic acid (VII) was coupled with morpholine (VIII) using EDC to furnish the title morpholide.