Traxanox sodium, Y-12141, Clearnal
四唑吡色酮Chemical Name: 9-Chloro-5-oxo-7-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3-b]pyridine sodium salt pentahydrate; 9-Chloro-7-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3,-b]pyridin-5-one sodium salt pentahydrate
CAS No. 58712-69-9 (free anhydrous acid)
项目整合开发状态: Phase III
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:This compound can be prepared by two related ways:1) The condensation of 2-chloronicotinic acid (I) with 3-chloro-4-hydroxybenzonitrile (II) by means of sodium methoxide in nitrobenzene at 180 C gives 2-(2-chloro-4-cyanophenoxy)nicotinic acid (III),which by reaction with sodium azide in DMF at 100 C is converted into 2-[2-chloro-4(1H)-tetrazol-5-yl)phenoxy]nicotinic acid (IV).Finally,this compound is cyclized with H2SO4 at 180 C.2) The cylization of gives 2-(2-chloro-4-cyanophenoxy)nicotinic acid (III) with H2SO4 at 180 C gives 9-chloro-5-oxo-5H-[1]benzopyrano[2,3]pyridine-4-carbonitrile (V) ,which is then treated with sodium azide.
📌 参考资料/链接：
参考文献标题:Y-12141
文献作者:Castar,J.; Hillier,K.
参考来源:Drugs Fut 1980,5(5),261
📄 详细内容
合成路线:This compound can be prepared by two related ways:1) The condensation of 2-chloronicotinic acid (I) with 3-chloro-4-hydroxybenzonitrile (II) by means of sodium methoxide in nitrobenzene at 180 C gives 2-(2-chloro-4-cyanophenoxy)nicotinic acid (III),which by reaction with sodium azide in DMF at 100 C is converted into 2-[2-chloro-4(1H)-tetrazol-5-yl)phenoxy]nicotinic acid (IV).Finally,this compound is cyclized with H2SO4 at 180 C.2) The cylization of gives 2-(2-chloro-4-cyanophenoxy)nicotinic acid (III) with H2SO4 at 180 C gives 9-chloro-5-oxo-5H-[1]benzopyrano[2,3]pyridine-4-carbonitrile (V) ,which is then treated with sodium azide.
参考文献标题:
文献作者:Ohe,T.; Tsuruda,M.
参考来源:US 4085111
合成路线:This compound can be prepared by two related ways:1) The condensation of 2-chloronicotinic acid (I) with 3-chloro-4-hydroxybenzonitrile (II) by means of sodium methoxide in nitrobenzene at 180 C gives 2-(2-chloro-4-cyanophenoxy)nicotinic acid (III),which by reaction with sodium azide in DMF at 100 C is converted into 2-[2-chloro-4(1H)-tetrazol-5-yl)phenoxy]nicotinic acid (IV).Finally,this compound is cyclized with H2SO4 at 180 C.2) The cylization of gives 2-(2-chloro-4-cyanophenoxy)nicotinic acid (III) with H2SO4 at 180 C gives 9-chloro-5-oxo-5H-[1]benzopyrano[2,3]pyridine-4-carbonitrile (V) ,which is then treated with sodium azide.
参考文献标题:
文献作者:Ohe,T.; Tsuruda,M.
参考来源:JP 76113899
产品链接: CAS No. 58712-69-9››