2614W94-药物合成数据库

【药物名称】2614W94

化学结构式(Chemical Structure):

参考文献No.	39104
标题:	Pharmacologically active cpds. and use
作者:	Boros, E.; Harfenist, M.; Heyer, D. (Krenitsky Pharmaceuticals, Inc.)
来源:	WO 9812190

合成路线图解说明: The condensation of 2-hydroxythiophenol (I) with 2,5-difluoronitrobenzene (II) in the presence of potassium tert-butoxide in DMF afforded 3-fluorophenoxathiin (III), which was oxidized to the sulfone (IV) using H2O2 and trifluoroacetic acid. Displacement of the fluorine atom of (IV) by 1,1,1-trifluoro-2-propanol (V) employing either KH in DMF or NaH in DMA then furnished the title compound.

合成路线图解说明: The condensation of 2-hydroxythiophenol (I) with 2,5-difluoronitro-benzene (II) in the presence of potassium tert-butoxide in DMF afforded 3-fluorophenoxathiin (III), which was oxidized to the sulfone (IV) using H2O2 and trifluoroacetic acid. Displacement of the fluorine atom of (IV) by 2,2,2-trifluoroethanol (V) employing either KH in DMF or KOt-Bu in acetonitrile then furnished the title compound.

合成路线图解说明: The condensation of 2-hydroxythiophenol (I) with 2,5-difluoronitro-benzene (II) in the presence of potassium tert-butoxide in DMF afforded 3-fluorophenoxathiin (III), which was oxidized to the sulfone (IV) using H2O2 and trifluoroacetic acid. Displacement of the fluorine atom of (IV) by 1,1,3,3-tetrafluoro-2-propanol (V) employing either KH in DMF or KOt-Bu in acetonitrile then furnished the title compound.