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【结 构 式】

【药物名称】Nicaraven, AVS, Antevas

【化学名称】1,2-Bis(nicotinamido)propane
      N-N'-(1-Methyl-1,2-ethanediyl)bis-3-pyridinecarboxamide

【CA登记号】79455-30-4

【 分 子 式 】C15H16N4O2

【 分 子 量 】284.32037

【开发单位】Chugai (Originator), Novartis (Comarketer)

【药理作用】Cerebrovascular Diseases, Treatment of, NEUROLOGIC DRUGS, Stroke, Treatment of, Free Radical Scavengers, Lipid Peroxidation Inhibitors

合成路线1

This compound can be obtained by three different ways: 1) By condensation of nicotinoyl chloride (I) with 1,2-diaminopropane (IV) by means of triethylamine in pyridine. 2) By reaction of nicotinic acid (II) with 1,2-diaminopropane (IV) by means of ethyl chloroformate and triethylamine in THF. 3) By heating at 120 C a mixture of methyl nicotinate (III) with 1,2-diaminopropane (IV).

1 Mori, T.; Takaku, S.; Matsuura, F.; Murakami, Y.; Noda, Y.; Yamazaki, T.; Neichi, T.; Nakakimura, H.; Kataoka, S (Chugai Pharmaceutical Co. Ltd.); Nicotinamide derivative, process dor preparing the same and pharmaceutical composition containing the same. EP 0029602; JP 56075474 .
2 Grau, M.; Serradell, M.N.; Castaner, J.; Blancafort, P.; AVS. Drugs Fut 1983, 8, 6, 485.
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) 10753 Nicotinoyl chloride C6H4ClNO 详情 详情
(II) 10752 Nicotinic acid; Niacin 59-67-6 C6H5NO2 详情 详情
(III) 13980 methyl nicotinate; Nicotinic acid, methyl ester 93-60-7 C7H7NO2 详情 详情
(IV) 30691 1,2-propanediamine; 2-amino-1-methylethylamine 78-90-0 C3H10N2 详情 详情
Extended Information