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他司美琼(tasimelteon,1)商品名为Hetlioz;化学名称:N-[[(1R,2R)-2-(2,3-二氢-4-苯并呋喃基)环丙基]甲基]丙酰胺;分子式:C_(15)H_(19)NO_2;CAS登记号:609799-22-6。它是一种新型褪黑素受体激动剂,最先被Bristol-Myers Squibb公司发现,后由Vanda制药公司继续研发,被开发用于治疗失眠、昼夜节律相关的睡眠障碍和抑郁~([1])。2014年1月31日,他司美琼被FDA批准上市,成为首个治疗盲人非24 h睡眠/觉醒紊乱症的药物~([1])。本文根据不同的起始原料及关键中间体,综述了他司美琼的合成路线(图1)。
Hismetamis (tasimelteon, 1) trade name is Hetlioz; chemical name: N - [[(1R, 2R) -2- (2,3- dihydro-4-benzofuranyl) cyclopropyl] methyl ] Propanamide Molecular formula: C_ (15) H_ (19) NO_2; CAS Registry Number: 609799-22-6. It is a novel melatonin receptor agonist, first discovered by Bristol-Myers Squibb and subsequently developed by Vanda Pharmaceuticals and developed for the treatment of insomnia, circadian rhythm related sleep disorders and depression. ]). On January 31, 2014, his company, Mei Qiong, was approved by the FDA for listing and became the first drug to treat non-24-h sleep / wake disorders in blind people. [1] In this paper, based on different starting materials and key intermediates, synthesis of methimax synthesis route (Figure 1).