CAS: 27912-14-7; Levobunolol Hydrochloride

该化合物是一种有选择性的β1-Anergy受体对抗剂,以其在管理高血压和青光眼方面的功效而著称. 它提供了一种有利的治疗指数,对心血管系统的影响最小. 它的选择性行动最大限度地减少了支气管运动的潜力,使其适合哮喘病人. 盐酸Levobunol是寻求平衡治疗选择的临床医生的可靠选择.

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合成工艺路线路线简述

    📜5-羟基-1-四氢萘酮,(S)-N-(1,1-二甲基乙本)-环氧基甲胺置于sodium Ethanolate体系中,用 甲醇,水 用作溶剂,化学反应 5.0H,以87.3%的收率获得盐酸左布诺洛尔
    参考文献:一种盐酸左布诺洛尔的制备方法
    标题:一种盐酸左布诺洛尔的制备方法
    摘要:本发明提供了一种盐酸左布诺洛尔的制备方法,本发明采用s‑1‑叔丁基‑环氧基甲基胺与5‑羟基‑1‑四氢萘酮进行取代反应,经酸化处理后制备得到目标产物盐酸左布诺洛尔.本发明提供的方法大大提升了反应的区域选择性,避免发生副反应,有效提高了盐酸左布诺洛尔的收率和光学纯度,收率达87.3%,Ee值超过99%.

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    专利信息


    专利号:US-9745419-B2
    优先权日:2014-01-24
    标 题 :Aqueous polyglycidol synthesis with ultra-low branching
    发明人:HARTH EVA M; SPEARS BENJAMIN R
    权利人:UNIV VANDERBILT
    摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for a variety of applications, including, but not limited to, drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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    主要参考文献


    1: Argikar UA, Dumouchel JL, Dunne CE, Saran C, Cirello AL, Gunduz M. Ocular Metabolism of Levobunolol: Historic and Emerging Metabolic Pathways. Drug Metab Dispos. 2016 Aug;44(8):1304-12. doi: 10.1124/dmd.116.070458. Epub 2016 May 17. doi: 10.1016/j.ophtha.2015.09.005. Epub 2015 Oct 31. Review.
    3: Horcajada-Reales C, Rodríguez-Soria VJ, Suárez-Fernández R. Allergic contact dermatitis caused by timolol with cross-sensitivity to levobunolol. Contact Dermatitis. 2015 Dec;73(6):368-9. doi: 10.1111/cod.12448. Epub 2015 Jul 31. eCollection 2015.
    5: Krishnamurthy R, Senthil S, Garudadri CS. Late postoperative choroidal detachment following an uneventful cataract surgery in a patient on topical latanoprost. BMJ Case Rep. 2015 Jul 14;2015. pii: bcr2015211408. doi: 10.1136/bcr-2015-211408. doi: 10.1016/j.amjmed.2014.12.005. Epub 2015 Jan 5. doi: 10.2147/CIA.S69420. eCollection 2014.

    合成参考文献


    摘要:American Heart Journal., 127(689), 1994 []
    参考文献:10.1007/s004170100312
    摘要:Melena J, Stanton D, Osborne NN. Comparative effects of antiglaucoma drugs on voltage-dependent calcium channels. Graefe's Archive for Clinical and Experimental Ophthalmology. 2001 Jul 03;239(7):522–30. doi: 10.1007/s004170100312.
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