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One-pot synthesis of 2-trifluoromethyl and 2-difluoromethyl substituted benzo-1,3-diazoles
Tetrahedron Letters ( IF 1.5 ) Pub Date : 30 April 2007 , DOI: 10.1016/j.tetlet.2007.03.015
Fenglian Ge , Zengxue Wang , Wen Wan , Wencong Lu , Jian Hao

2-Trifluoromethyl and 2-difluoromethyl substituted benzimidazole, benzoxazole and benzothiazole derivatives were efficiently prepared through a one-pot reaction of trifluoroacetic acid and difluoroacetic acid, respectively, with commercially available o-phenylenediamines, 2-aminophenols, and 2-aminobenzenethiols in good to excellent yields. Subsequential bromination of 2-difluoromethyl groups by photolysis with NBS led to the formation of bromodifluoromethyl benzo-1,3-diazoles which may be utilized to prepare the new generation of gem-difluoromethylene linked identical or non-identical twin molecules for drug synthesis.

中文翻译:

一锅合成2-三氟甲基和2-二氟甲基取代的苯并-1,3-二唑

通过三锅法分别将三氟乙酸和二氟乙酸与市售的苯二胺,2-氨基酚和2-氨基苯硫醇进行一锅反应,可有效地制备2-三氟甲基和2-二氟甲基取代的苯并咪唑,苯并恶唑和苯并噻唑衍生物。优异的产量。通过NBS光解法对2-二氟甲基进行的后续溴化反应导致形成溴二氟甲基苯并-1,3-二唑,可用于制备新一代的与宝石-二氟亚甲基连接的相同或不同的双分子用于药物合成。
更新日期:2017-01-31
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