CAS: 69049-06-5; Alfentanil Hydrochloride

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alfentanil N-[4-(methoxymethyl)-4-piperidinyl]-N-phenylpropanamide 2-(4-ethyl-4,5-dihydro-5-oxo-1H-tetrazol-1-yl)ethyl bromide

合成工艺路线路线简述

    📜阿芬太尼置于盐酸体系中,用 甲醇,水 作为反应溶剂,化学反应生成 盐酸阿芬他尼
    参考文献:一种利用连续流微通道反应器制备苯胺基哌啶类药物的合成方法
    标题:一种利用连续流微通道反应器制备苯胺基哌啶类药物的合成方法
    摘要:本发明公开了一种利用连续流微通道反应器制备苯胺基哌啶类药物的合成方法.该方法通过控制物料流速和连续流微通道反应器各模块的温度,能有效提高苯胺基哌啶类药物最后一步合成的反应选择性和转化率.在此基础上,反应液经过简单的提取,浓缩操作后,有机溶剂溶解浓缩剩余物,加入相应的酸成盐,析晶,过滤,得到该药物的酸式盐粗品,再经过脱色和重结晶得到相应的酸式盐.此方法提供了一种利用连续流微通道反应器进行苯胺基哌啶类药物合成的途径,提高了反应的转化率和选择性,降低了杂质含量,简化了成盐精制步骤,提高产物收率,同时使产物纯度均达到99.8%以上.

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    专利信息


    专利号:US-7208604-B2
    优先权日:1999-12-06
    标题 :Methods for the synthesis of alfentanil, sufentanil, and remifentanil
    发明人:MATHEW JACOB; KILLGORE J KENDALL
    权利人:MALLINCKRODT INC
    摘要:Synthetic pathways are disclosed for synthesizing derivatives or analogs of fentanyl. Specifically set out are pathways for synthesizing alfentanil, sufentanil and remifentanil. The disclosed methods require fewer steps and produce a greater yield of product than methods reported in the prior art.

    专利号:US-2006149071-A1
    优先权日:1999-12-06
    标 题 :New methods for the synthesis of alfentanil, sufentanil, and remifentanil

    专利号:US-5728695-A
    优先权日:1994-12-23
    标题 :Spiroketal derivatives, compositions containing them and their use as therapeutic agents
    发明人:HARRISON TIMOTHY; OWEN SIMON NEIL; SEWARD EILEEN MARY; SWAIN CHRISTOPHER JOHN
    权利人:MERCK SHARP & DOHME
    摘要:The present invention relates to spiroketal derivatives of formula (I) and pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 9a , R 9b , m and n are as defined in the specification, and to processes for their preparation, to intermediates used in their synthesis, to pharmaceutical compositions containing them, and to their use in therapy. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

    专利号:CN-101208345-B
    优先权日:2005-05-25
    标 题 :(S) -N-methylnaltrexone, method of synthesis and pharmaceutical use thereof

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.2165/00003495-199651050-00002
    摘要:Cherny NI. Opioid analgesics: comparative features and prescribing guidelines. Drugs. 1996 May;51(5):713–37. doi: 10.2165/00003495-199651050-00002.
    参考文献:10.2165/00003495-199651050-00005
    摘要:Bhatt-Mehta V. Current guidelines for the treatment of acute pain in children. Drugs. 1996 May;51(5):760–76. doi: 10.2165/00003495-199651050-00005.
    参考文献:10.1007/bf00449683
    摘要:Meert TF. Pharmacotherapy of opioids: present and future developments. International Journal of Clinical Pharmacy. 1996 Jan;18(1):1–15. doi: 10.1007/bf00449683.
    参考文献:10.1007/bf02942789
    摘要:Taylor A, Phelan D, McCarthy JR. Pain relief following cardiac surgery: A review. Irish Journal of Medical Science. 1996 Jan;165(1):1–6. doi: 10.1007/bf02942789.
    参考文献:10.1007/bf02246641
    摘要:Butelman ER, Negus SS, Lewis JW, Woods JH. Clocinnamox antagonism of opioid suppression of schedule-controlled responding in rhesus monkeys. Psychopharmacology (Berl). 1996 Feb;123(4):320–4. doi: 10.1007/bf02246641.
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