CAS: 62-67-9; (4R,4Ar,7S,7Ar,12Bs)-3-Prop-2-Enyl-2,4,4A,7,7A,13-Hexahydro-1H-4,12-Methanobenzofuro[3,2-E]Isoquinoline-7,9-Diol

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CAS号106-95-6 烯丙基溴 | CAS号466-97-7 去甲吗啡 | CAS号58229-59-7 17-allyl-4,5α-e... | CAS号57934-01-7 4,5α-epoxy-3,6α...

📜4,5α-Epoxy-3,6α-Bis-Vinyloxycarbonyloxy-Morphin-7-Ene; Hydrobromide置于盐酸,Sodium Carbonate体系中,用 乙醇 作为反应溶剂,化学反应 6.0H,反应生成 烯丙吗啡
参考文献:Value Of The Vinyloxycarbonyl Unit In Hydroxyl Protection: Application To The Synthesis Of Nalorphine
标题:Value Of The Vinyloxycarbonyl Unit In Hydroxyl Protection: Application To The Synthesis Of Nalorphine
摘要:
DOI:10.1016/s0040-4039(01)93105-3

专利信息

专利号:US-2012165520-A1
优先权日:2010-12-23
标题:Process for the synthesis of prodrugs of opioids
发明人：MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.

专利号:US-5668285-A
优先权日:1986-10-31
标 题 :Total synthesis of northebaine, normophine, noroxymorphone enantiomers and derivatives via N-Nor intermediates
发明人：RICE KENNER CRALLE; NEWMAN AMY HAUCK
权利人:US HEALTH
摘要:The invention involves a method of making key intermediates useful in the synthesis of many opiate narcotics and antagonists and agonists; and the non-opiate enantiomers thereof which have potent antitussive properties. The synthesis starts from either the natural or unnatural enantiomer of nordihydrocodeinone and produces 8, 14-dihydronorthebaine, the diketal of 7-bromonordihydrocodeinone, northebaine, norcodeinone diketal and 14-hydroxynorcodeinone intermediates without the necessity of leaving the N-nor structure. The syntheses have fewer steps than previous methods, and also have high yields.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-8106201-B2
优先权日:2003-09-22
标 题:Process for the synthesis of morphinane compounds and intermediates thereof
发明人：SMITH CRAIG; PURCELL STUART; WADDELL LUCY; HAYES NICHOLAS; RITCHIE JARROD; HALLIDAY SCOTT BRIAN; MITCHELL MELVILLE; WILSON GEORGE SCOTT
权利人:SMITH CRAIG; PURCELL STUART; WADDELL LUCY; HAYES NICHOLAS; RITCHIE JARROD; HALLIDAY SCOTT BRIAN; MITCHELL MELVILLE; WILSON GEORGE SCOTT; JOHNSON MATTHEY PLC; GLAXOSMITHKLINE AUSTRALIA PTY LTD
摘要:This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates and to processes which utilise such intermediates in the synthesis of morphinane compounds.

专利号:EP-0496830-B1
优先权日:1989-10-16
标 题 :Total synthesis of northebaine, normorphine, noroxymorphone enantiomers and derivatives via n-nor intermediates
发明人：RICE KENNER CRALLE; NEWMAN AMY HAUCK
权利人:US HEALTH
摘要:Families of antagonist-agonists and opiate narcotics are produced from norhydrocodeinone. In a preferred embodiment, norhydrocodeinone is refluxed with sulfosalicyclic dimethylketal and delta-6-enol ether derivatives and is then converted entirely to the ether by the addition of dry tetrahydrofuran simultaneously with the removal of the thus produced ether. The ether is then reacted with methanesulfonic acid and N-bromoacetamide to form the hydrobromide salt of the 7-bromodimethylketal derivative. From this derivative, a variety of products can be derived, including the novel further intermediate 14 hydroxynorcodeinone. The present invention enables derivation using a starting material which, unlike the starting materials of prior art processes, is available in the natural (-) or synthetic (+) form. Thus, the method of the present invention provides the only known route for the synthesis of (+) forms of various derivatives and intermediates, such as (+)-7-bromo-dimethylketal nordihydrocodeinone.

专利号:US-9597327-B2
优先权日:2005-05-25
标 题:Synthesis of (R)-N-methylnaltrexone
发明人：DOSHAN HAROLD D; PEREZ JULIO
权利人:PROGENICS PHARM INC
摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.