VUF-K-9015
Chemical Name: 7-[3-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-ylmethoxy]benzyloxy]-3,4-dihydro-2H-1,4-benzothiazin-3-one
CAS No. 198012-83-8
项目整合开发状态: Biological Testing
项目研究机构: Kowa (Originator), Vrije Universiteit (Originator)
合成路线:Alkylation of 3-hydroxybenzyl alcohol (II) with 2-chloromethylquinazoline (I) in the presence of K2CO3 and tetrabutylammonium bromide provided ether (III).The hydroxyl group of (III) was converted to chloride (IV) by treatment with thionyl chloride.Finally,alkylation of hydroxybenzothiazinone (V) with chloride (IV) yielded the title compound.
合成路线:Alkylation of 3-hydroxybenzyl alcohol (II) with benzimidazolylmethyl chloride (I) in the presence of K2CO3 and tetrabutylammonium bromide provided ether (III).The hydroxyl group of (III) was converted to chloride (IV) by treatment with thionyl chloride.Finally,alkylation of hydroxybenzothiazinone (V) with chloride (IV) yielded the title compound.
📌 参考资料/链接：
参考文献标题:Heteroaryl substd.phenylene derivs.,their preparation and their use a leukotriene receptor antagonists
文献作者:Timmerman,H.; Zhang,M.; Onogi,K.; Tamura,M.; Toma,T.; Wada,Y.(Kowa Co.,Ltd.)
参考来源:EP 0799826; JP 1997323975; US 5756518; US 5885987; US 6011033
📄 详细内容
合成路线:Alkylation of 3-hydroxybenzyl alcohol (II) with 2-chloromethylquinazoline (I) in the presence of K2CO3 and tetrabutylammonium bromide provided ether (III).The hydroxyl group of (III) was converted to chloride (IV) by treatment with thionyl chloride.Finally,alkylation of hydroxybenzothiazinone (V) with chloride (IV) yielded the title compound.
合成路线:Alkylation of 3-hydroxybenzyl alcohol (II) with benzimidazolylmethyl chloride (I) in the presence of K2CO3 and tetrabutylammonium bromide provided ether (III).The hydroxyl group of (III) was converted to chloride (IV) by treatment with thionyl chloride.Finally,alkylation of hydroxybenzothiazinone (V) with chloride (IV) yielded the title compound.
参考文献标题:VUF-K-8707 and analogs,non-acidic leukotriene D4 receptor antagonists
文献作者:Tamura,M.; Tohma,T.; Onogi,K.; et al.
参考来源:15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998,Edinburgh) 1998,Abst P.226