Tocainide hydrochloride, Tonocard
2-氨基-N-(2,6-二甲基苯基)丙酰胺Chemical Name: 2-Amino-N-(2,6-dimethylphenyl)propanamide hydrochloride
CAS No. 41708-72-9 (free base)
项目整合开发状态: Launched-1981
项目研究机构: AstraZeneca (Originator), Merck & Co. (Originator)
合成路线:Compound can be prepared in two different ways both starting from 2,6-xylidine (I):1) By condensation of (I) with N-carbobenzoxyalanine (B) by means of dicyclohexylcarbodiimide in methylenechloride giving N-(carbobenzoxyalanyl)xylidine (II),which is then hydrogenated over Pd/C in ethanol - methylene chloride.2) By condensation of (I) with 2-bromopropionyl bromide (A) by means of sodium acetate in acetic acid giving 2-bromo-2',6'-propionoxylidide (III),which is then treated with NH3 in alcohol water.
📌 参考资料/链接：
参考文献标题:Tocainide
文献作者:Hillier,K.; Castar,J.
参考来源:Drugs Fut 1977,2(2),141
📄 详细内容
合成路线:Compound can be prepared in two different ways both starting from 2,6-xylidine (I):1) By condensation of (I) with N-carbobenzoxyalanine (B) by means of dicyclohexylcarbodiimide in methylenechloride giving N-(carbobenzoxyalanyl)xylidine (II),which is then hydrogenated over Pd/C in ethanol - methylene chloride.2) By condensation of (I) with 2-bromopropionyl bromide (A) by means of sodium acetate in acetic acid giving 2-bromo-2',6'-propionoxylidide (III),which is then treated with NH3 in alcohol water.
参考文献标题:Primary amino acylanilides methods of making the same and use as antiarrhythmic drugs
文献作者:Boyes,R.N.; et al.
参考来源:DE 2400540; ES 422085; FR 2213065; GB 1461602; JP 49116034
合成路线:Compound can be prepared in two different ways both starting from 2,6-xylidine (I):1) By condensation of (I) with N-carbobenzoxyalanine (B) by means of dicyclohexylcarbodiimide in methylenechloride giving N-(carbobenzoxyalanyl)xylidine (II),which is then hydrogenated over Pd/C in ethanol - methylene chloride.2) By condensation of (I) with 2-bromopropionyl bromide (A) by means of sodium acetate in acetic acid giving 2-bromo-2',6'-propionoxylidide (III),which is then treated with NH3 in alcohol water.
参考文献标题:Propionamide derivative a method of making it and therapeutic compositions containing it
文献作者:Boyes,R.N.; et al.
参考来源:DE 2235745; FR 2147277; GB 1374367; NL 7210418
产品链接: CAS No. 41708-72-9››