Ameltolide, ADD-75073, LY-201116, -Drug Synthesis Database

【结构式】

【药物名称】Ameltolide, ADD-75073, LY-201116

【化学名称】4-Amino-N-(2,6-dimethylphenyl)benzamide

【CA登记号】787-93-9, 107293-98-1 (monoHCl)

【分子式】C₁₅H₁₆N₂O

【分子量】240.30757

【开发单位】Lilly (Originator)

【药理作用】Antiarrhythmic Drugs, Antiepileptic Drugs, CARDIOVASCULAR DRUGS, NEUROLOGIC DRUGS

合成路线1

4-Nitrobenzoylchloride (I) is condensed with 2,6-dimethylaniline (II) in the presence of base (potassium carbonate or triethylamine) to provide the 4-nitrobenzamide (III). Reduction of the aromatic nitro group in (III) using catalytic hydrogenation produces the corresponding 4-aminobenzamide, ameltolide.

参考文献中间体

【1】 Clark, C.R.; Robertson, D.W.; Leander, J.D.; AMELTOLIDE. Drugs Fut 1990, 15, 10, 983.
【2】 Clark, C.R.; Sansom, R.T.; Lin, C.-M.; Norris, G.N.; Anticonvulsant activity of some 4-aminobenzanilides. J Med Chem 1985, 28, 9, 1259.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	18941	p-nitrobenzoyl chloride; 4-nitrobenzoyl chloride	122-04-3	C₇H₄ClNO₃	详情	详情
(II)	17527	2,6-Xylidine; 2,6-Dimethylaniline; 2,6-Dimethylphenylamine	87-62-7	C₈H₁₁N	详情	详情
(III)	31178	N-(2,6-dimethylphenyl)-4-nitrobenzamide		C₁₅H₁₄N₂O₃	详情	详情

Extended Information