CAS: 33522-95-1; Nor Oxymorphone

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CAS号465-65-6 纳洛酮 | CAS号76-41-5 氢羟吗啡酮 | CAS号144333-31-3 14-acetylnoroxy... | CAS号36397-12-3 N-desmethyl-N-c... | CAS号76-57-3 可待因 | CAS号465-65-6 纳洛酮 | CAS号2183-56-4 氢吗啡醇 | CAS号342884-62-2 (4BS,8R,8AS,14B... | CAS号16590-41-3 纳曲酮 | CAS号16676-29-2 盐酸纳曲酮

吗啡置于甲酸,草酰氯,硫酸,Palladium On Activated Charcoal,氢气,双氧水,Sodium Acetate,Potassium Hydrogencarbonate,溶剂黄146,二甲基亚砜体系中,用 乙醇,二氯甲烷,水,乙酸酐,异丙醇 用作溶剂,-80.0~90.0 °C,1.0 Mpa 条件下,反应 37.5H,反应生成14-羟基二氢降吗啡酮盐酸盐
参考文献:Novel Synthesis Of Noroxymorphone From Morphine
标题:Novel Synthesis Of Noroxymorphone From Morphine
摘要:本发明涉及一种改进的过程,将吗啡转化为诺罗西莫酮,包括以下步骤:将式(va)或(vb)的化合物 分别反应为式(via)或(vlb)的化合物,其特征在于,所述反应通过过氧化氢和有机酸进行的,其中所述有机酸和过氧化氢混合并在加入式(v)的化合物之前允许反应一定的感应时间.

专利信息

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-10927122-B2
优先权日:2017-12-05
标 题:Synthesis of noroxymorphone
发明人：SANTANDREA ERNESTO; WEBER BEAT THEODOR; BOUDIER ANDREAS; GEISELER OLIVER; JEGER PATRICK
权利人:SIEGFRIED AG
摘要:The present invention relates to the improved synthesis of noroxymorphone of formula (III). Particularly, the invention shows a way how to reduce the impurity level in the product avoiding lengthy purification steps.

专利号:US-8461384-B2
优先权日:2006-12-11
标 题 :Preparation of amides from an acid and amine for intermediates in the synthesis of morphinans
发明人：WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L
权利人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L; MALLINCKRODT LLC
摘要:The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl 3 that is necessary to form the 3,4-dihydroisoquinoline.

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-6013796-A
优先权日:1996-07-26
标 题:Preparation of naltrexone from codeine and 3-benzylmorphine
发明人：HUANG BAO-SHAN; LU YANSONG; JI BEN-YI; CHRISTODOULOU ARIS P
权利人:PENICK CORP
摘要:For the synthesis of 3-methylnaltrexone from codeine in this invention, codeine is converted to 6-acetylcodeine, which is N-demethylated to 6-acetylcodeine hydrochloride, followed by alkylating the nitrogen to form 17-cyclopropylmethylnorcodeine. The latter is oxidized to 17-cyclopropylmethylnorcodeinone. For the synthesis of naltrexone from morphine in this invention, morphine is converted to 3-benzylnormorphine as described above in the synthesis of noroxymorphone. 3-Benzylnormorphine is reacted with cyclopropylmethyl halide to produce 3-benzyl-17cyclopropylmethylnormorphine, a novel compound, which is oxidized to 3-benzyl-17-cyclopropylmethyl-normorphinone, a novel compound, by Swern oxidation.

专利号:US-2023357257-A1
优先权日:2020-12-28
标 题 :Novel process for the synthesis of noroxymorphone from morphine
发明人：GORBACHEV DMITRY; LAM HON WAI; SAXENA AAKARSH; SAXENA NAVIN SATYAPAL
权利人:NAVIN SAXENA RESEARCH & TECH PVT LTD
摘要:The present invention relates to a novel, efficient, pot- and atom-economical, and industrially applicable process for converting morphine to noroxymorphone using reagents and solvents of lesser toxicity and lower cost with respect to those used in the prior art.