MD-39-AM
2-甲硫基-N-苯基吡啶并[3,2-e]嘧啶-4-胺Chemical Name: 2-(Methylsulfanyl)-4-(phenylamino)pyrido[2,3-d]pyrimidine hydrochloride
CAS No. 72564-74-0 (free base)
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The synthesis of MD-39-AM (V) was carried out as follows:From 2-chloronicotinic acid (as its acyl chloride) (I) and thiourea in triethylamine (1:1:2),compound (II) was obtained.However,in order to avoid the substitution of 2-Cl by sulfur,2-methylisothiourea was used.By boiling a solution of (II) in dimethylformamide (DMF) for 15 min,(III) (87%) was obtained.Reaction of (III) with phosphorous oxychloride gave 4-chloro-2-(methylthio)pyrido[2,3-d]pyrimidine (IV) (90%).By reacting (IV) with aniline in ethanol,MD-39-AM was obtained.
📌 参考资料/链接：
参考文献标题:Diuretic and hypotensive activities of 4-anilino derivatives of 2-methylthiopyrido[2,3-d]pyrimidines
文献作者:Ochoa,M.C.; Fern醤dez,F.J.; Sanmart韓,C.; Monge,A.; Mart韓ez-Merino,V.; Bellver,C.; Artigas,P.
参考来源:Arzneim-Forsch Drug Res 1990,40(11),1230-3
📄 详细内容
合成路线:The synthesis of MD-39-AM (V) was carried out as follows:From 2-chloronicotinic acid (as its acyl chloride) (I) and thiourea in triethylamine (1:1:2),compound (II) was obtained.However,in order to avoid the substitution of 2-Cl by sulfur,2-methylisothiourea was used.By boiling a solution of (II) in dimethylformamide (DMF) for 15 min,(III) (87%) was obtained.Reaction of (III) with phosphorous oxychloride gave 4-chloro-2-(methylthio)pyrido[2,3-d]pyrimidine (IV) (90%).By reacting (IV) with aniline in ethanol,MD-39-AM was obtained.
参考文献标题:MD-39-AM
文献作者:Mart韓ez-Merino,V.; Monge,A.; Sanmart韓,C.
参考来源:Drugs Fut 1992,17(2),107
合成路线:The synthesis of MD-39-AM (V) was carried out as follows:From 2-chloronicotinic acid (as its acyl chloride) (I) and thiourea in triethylamine (1:1:2),compound (II) was obtained.However,in order to avoid the substitution of 2-Cl by sulfur,2-methylisothiourea was used.By boiling a solution of (II) in dimethylformamide (DMF) for 15 min,(III) (87%) was obtained.Reaction of (III) with phosphorous oxychloride gave 4-chloro-2-(methylthio)pyrido[2,3-d]pyrimidine (IV) (90%).By reacting (IV) with aniline in ethanol,MD-39-AM was obtained.
参考文献标题:2-Arylamino-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidines: Synthesis and diuretic activity
文献作者:Mart韓ez-Merino,V.; Ochoa,M.C.; Fern醤dez,F.J.; Artigas,P.; Monge,A.; Bellver,C.; Sanmart韓,C.; Fern醤dez-羖varez,E.
参考来源:Eur J Med Chem 1989,24209
产品链接: CAS No. 72564-74-0››