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项目整合精选>>>Tizanidine hydrochloride, DS-103282 ch, AN-021A, DS-103282, Zanaflex, Ternelin, Sirdalud
Tizanidine hydrochloride, DS-103282 ch, AN-021A, DS-103282, Zanaflex, Ternelin, Sirdalud
盐酸替扎尼定 替扎尼定 Chemical Name: 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole hydrochloride; 5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazole hydrochloride
CAS No. 64461-82-1, 51322-75-9 (free base)
项目整合开发状态: Launched-1984
项目研究机构: Novartis (Originator), Acorda (Licensee), Draxis Health (Licensee), Elan (Licensee), Shire Pharmaceuticals (Licensee)
合成路线:4-Amino-5-chloro-2,1,3-benzothiadiazole (I) is reacted with CSCl2 to 5-chloro-4-isothiocyano-2,1,3-benzothiadiazole (II),which gives 4-[3-(2-aminoethyl)-2-thioureido]-5-chloro-2,1,3-benzothiadiazole (IV) with 1,2-diaminoethane (III).Cyclization in methanol in the presence of KOH/Pb(OAc)2 leads after 1 h at reflux to DS 103-282.
📌 参考资料/链接：
参考文献标题:DS-103-282
文献作者:Unterhalt,B.
参考来源:Drugs Fut 1980,5(1),27
📄 详细内容
合成路线:4-Amino-5-chloro-2,1,3-benzothiadiazole (I) is reacted with CSCl2 to 5-chloro-4-isothiocyano-2,1,3-benzothiadiazole (II),which gives 4-[3-(2-aminoethyl)-2-thioureido]-5-chloro-2,1,3-benzothiadiazole (IV) with 1,2-diaminoethane (III).Cyclization in methanol in the presence of KOH/Pb(OAc)2 leads after 1 h at reflux to DS 103-282.
参考文献标题:4-(2-Imidazolin-2-ylamino)-2,1,3-benzothiadizoles
文献作者:Neumann,P.; et al.
参考来源:CH 579565
合成路线:4-Amino-5-chloro-2,1,3-benzothiadiazole (I) is reacted with CSCl2 to 5-chloro-4-isothiocyano-2,1,3-benzothiadiazole (II),which gives 4-[3-(2-aminoethyl)-2-thioureido]-5-chloro-2,1,3-benzothiadiazole (IV) with 1,2-diaminoethane (III).Cyclization in methanol in the presence of KOH/Pb(OAc)2 leads after 1 h at reflux to DS 103-282.
参考文献标题:
文献作者:Becher,W.
参考来源:Private Communication 2002,Abst 1520
产品链接: CAS No. 64461-82-1›› 产品链接: CAS No.51322-75-9››