2614W94

3-[1-(三氟甲基)乙氧基]苯昔林-10,10-二氧化物Chemical Name: 3-[1-(Trifluoromethyl)ethoxy]phenoxathilin-10,10-dioxide
CAS No. 205187-35-5, 205187-51-5 ((R)-isomer), 205187-54-8 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Krenitsky (Originator)
合成路线: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: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: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.