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【结 构 式】

【药物名称】Lidamidine hydrochloride, WHR-1142A, Lidaral

【化学名称】1-(2,6-Dimethylphenyl)-3-methylamidino urea hydrochloride

【CA登记号】65009-35-0, 66871-56-5 (free base)

【 分 子 式 】C11H17ClN4O

【 分 子 量 】256.73734

【开发单位】Aventis Pharma (Originator), Yamanouchi (Originator), Valeant (Licensee)

【药理作用】Antidiarrheal Agents, GASTROINTESTINAL DRUGS

合成路线1

The reaction of 2,6-dimethylaniline (I) with phosgene (II) in refluxing benzene gives 2,6-dimethylphenyl isocyanate (III), which is then condensed with methylguanidine carbonate (A) by means of K2CO3 in THF and treated with HCl to obtain the corresponding hydrochloride.

1 Nouvelles amidinourees, leur preparation et leur emploi. BE 0844832 .
2 Roberts, P.J.; Castaner, J.; Lidamidine hydrochloride. Drugs Fut 1979, 4, 3, 206.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(A) 28411 N-Methylguanidine 598-12-9 C2H7N3 详情 详情
(I) 17527 2,6-Xylidine; 2,6-Dimethylaniline; 2,6-Dimethylphenylamine 87-62-7 C8H11N 详情 详情
(III) 29955 2,6-Dimethylphenyl isocyanate; 2-Isocyanato-1,3-dimethylbenzene 28556-81-2 C9H9NO 详情 详情
Extended Information