CAS: 14357-78-9; Diprenorphine,17-(Cyclopropylmethyl)-4,5-Epoxy-18,19-Dihydro-3-Hydroxy-6-Methoxy-α,α-Dimethyl-6,14-Ethenomorphinan-7-Methanol

上下游产品

CAS号1489-69-6 环丙甲醛 | CAS号2579-67-1 17-Northebaine | CAS号16528-12-4 (5R,6R,7S,9R,13... | CAS号74-88-4 碘甲烷 | CAS号72221-15-9 N-Benzyl-northebain

📜蒂巴因置于咪唑,Lithium Aluminium Tetrahydride,Sodium Hydride,Potassium Carbonate,1-丙烷硫醇钠体系中,用 四氢呋喃,四氯化碳,乙醚,N,N-二甲基甲酰胺 用作溶剂,化学反应 38.03H,反应生成地利洛非
参考文献:碳11标记的二肾上腺素的合成:用于鸦片受体正电子发射断层研究的放射性配体
标题:碳11标记的二肾上腺素的合成:用于鸦片受体正电子发射断层研究的放射性配体
摘要:3-[o--丁基二甲基甲硅烷基)-6-(o-去甲基)-二丙诺啡与[ 11 C]-甲基碘的选择性烷基化,然后进行去甲硅烷基化作用,制得在11-甲氧基位置标记的[ 11 C]-二丙诺啡,产率为10%.在30分钟的合成结束时,其比活度为1740 Mci /μmol.
Doi:10.1016/s0040-4039(01)83849-1

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-8273887-B2
优先权日:2008-09-30
标题:Processes for synthesis of opiate alkaloid derivatives
发明人：MANNINO ANTHONY; ZDRODOWSKI JAMES
权利人:MANNINO ANTHONY; ZDRODOWSKI JAMES; MALLINCKRODT LLC
摘要:The present invention provides processes for the synthesis of opiate alkaloids. In particular, the opiate alkaloids produced by the process of the invention are typically intermediate compounds that may be utilized to produce a variety of biologically active alkaloids including buprenorphine and diprenorphine.

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-8232396-B2
优先权日:2008-09-30
标题:Processes for the synthesis of opiates alkaloids with reduced impurity formation
发明人：ORR BRIAN; STEELE MIRANDA
权利人:ORR BRIAN; STEELE MIRANDA; MALLINCKRODT LLC
摘要:The invention provides processes for the production of opiate alkaloids. In particular, the present invention provides processes for the formation of opiate alkaloids that minimizes the formation of impurities.

专利号:US-8115002-B2
优先权日:2006-09-20
标 题:Preparation of substituted morphinan-6-ones and salts and intermediates thereof
发明人：WANG PETER X; MOSER FRANK W; CANTRELL GARY L; GROTE CHRISTOPHER W
权利人:WANG PETER X; MOSER FRANK W; CANTRELL GARY L; GROTE CHRISTOPHER W; MALLINCKRODT LLC
摘要:The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof.