Rilmazafone hydrochloride dihydrate, 450191-S, Rhythmy-药物合成数据库

【药物名称】Rilmazafone hydrochloride dihydrate, 450191-S, Rhythmy

化学结构式(Chemical Structure):

参考文献No.	66423
标题:	450191-S
作者:	Serradell, M.N.; Casta馿r, J.
来源:	Drugs Fut 1984,9(7),522

合成路线图解说明: The condensation of 2',5-dichloro-2-aminobenzophenone (I) with N,N-dimethyl-2-chloroacetoacetamide (II), by means of NaNO2 HCl in water acetone gives N,N-dimethyl-2-chloro-2-[2-(2-chlorobenzoyl)-5-chlorophenylazo]acetoacetamide (III), which by a treatment with aqueous NH3 in ethyl acetate is converted into N,N-dimethyl-2-amino-2-[2-(2-chlorobenzoyl)-5-chlorophenylazo]acetamide (IV). The cyclization of (IV) with phthalylglycylglycyl chloride (V) in THF-HMPT affords 2',5-dichloro-2-[3-dimethylcarbamoyl-5-(phthalylglycylaminomethyl)-1H-1,2,4-triazol-1-yl]benzophenone (VI), which is finally deprotected by a treatment with hydrazine in refluxing ethanol, and with HCl in the same solvent.

参考文献No.	800095
标题:	Synthesis and biological activity of (3,5-disubstituted-1H-1,2,4-triazol-1-yl)benzophenone derivatives
作者:	Ishiba, T.; Tsukinoki, Y.; Hirai, K.; Sugimoto, H.; Hirose, K.; Fujishita, T.
来源:	J Heterocycl Chem 1982,19(6),1363-9

合成路线图解说明: The condensation of 2',5-dichloro-2-aminobenzophenone (I) with N,N-dimethyl-2-chloroacetoacetamide (II), by means of NaNO2 HCl in water acetone gives N,N-dimethyl-2-chloro-2-[2-(2-chlorobenzoyl)-5-chlorophenylazo]acetoacetamide (III), which by a treatment with aqueous NH3 in ethyl acetate is converted into N,N-dimethyl-2-amino-2-[2-(2-chlorobenzoyl)-5-chlorophenylazo]acetamide (IV). The cyclization of (IV) with phthalylglycylglycyl chloride (V) in THF-HMPT affords 2',5-dichloro-2-[3-dimethylcarbamoyl-5-(phthalylglycylaminomethyl)-1H-1,2,4-triazol-1-yl]benzophenone (VI), which is finally deprotected by a treatment with hydrazine in refluxing ethanol, and with HCl in the same solvent.