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【结 构 式】 
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【药物名称】Pikamilone, LS-46432 【化学名称】N-Nicotinoyl-gamma-aminobutyric acid sodium salt 【CA登记号】62936-56-5 【 分 子 式 】C10H11N2NaO3 【 分 子 量 】230.20057 |
【开发单位】Russian Academy of Medical Sciences (Originator) 【药理作用】Anxiolytics, Cognition Disorders, Treatment of, NEUROLOGIC DRUGS, PSYCHOPHARMACOLOGIC DRUGS |
合成路线1
Nicotinic acid azide (I) is mixed with a solution of gamma-aminobutyric acid (II) in 1 N NaOH (pH 8-9). The mixture is stirred for 24 hours, evaporated and the residue is washed with methanol. The resultant sodium salt of nicotinoyl-gamma-aminobutyric acid is then dried. It can be further converted to nicotinoyl-gamma-aminobutyric acid (III) by dissolving in a minimum amount of water and adjusting pH to 3.5.
| 【1】 Kopelevich, V.M.; Trubnikov, V.I.; Shmvilovich, L.M.; et al. (USSR Res. Inst. Vitamins); Process for the preparation of N-nicotinoyl-gamma-aminoaliphatic acids or its esters. SU 325232 . |
| 【2】 Rejholec, V.; PIKAMILONE. Drugs Fut 1990, 15, 2, 133. |