CAS: 16676-29-2; Naltrexone Hydrochloride

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CAS号33522-95-1 14-羟基二氢降吗啡酮盐酸盐 | CAS号1489-69-6 环丙甲醛 | CAS号16590-41-3 纳曲酮 | CAS号111555-57-8 N-Methylnaltrindole | CAS号111555-58-9 NALTRIBEN MESYLATE | CAS号111555-53-4 Naltrindol | CAS号105618-26-6 去甲-BNI 二盐酸盐 | CAS号111469-81-9 纳曲吲哚盐酸盐 | CAS号16590-41-3 纳曲酮 | CAS号118111-54-9 Cyprodime hydro... | CAS号67875-55-2 1,3-双(1,1-二甲基乙基... | CAS号79798-39-3 酮啡诺

氢羟吗啡酮置于盐酸,硫酸,溶剂黄146,甲基磺酰氯,三乙胺体系中,用 水,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 39.0H,反应生成盐酸纳曲酮
参考文献: An Improved Process For The Preparation Of Morphinane Analogues[fr] Procédé Perfectionné Pour La Préparation D'Analogues De Morphinane
标题: An Improved Process For The Preparation Of Morphinane Analogues[fr] Procédé Perfectionné Pour La Préparation D'Analogues De Morphinane

专利信息

专利号:US-10654862-B2
优先权日:2015-03-18
标题 :Methods for the chemical synthesis of pyrrole-linked bivalent compounds, and compositions thereof
发明人：CRAN JOHN
权利人:AVEKSHAN LLC
摘要:The present invention in various aspects relates to the synthesis of pyrrole-linked bivalent compounds, including but not limited to norBNI, as well as pharmaceutical compositions comprising the same.

专利号:US-10022366-B2
优先权日:2013-04-23
标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery
发明人：STINCHCOMB AUDRA L; GHOSH PRIYANKA
权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND
摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

专利号:US-4089855-A
优先权日:1976-04-23
标题:Process for the stereoselective reduction of 6- and 8-keto morphine and morphinan derivatives with formamidinesulfinic acid and compounds obtained thereby
发明人：CHATTERJIE NITHIANANDA; INTURRISI CHARLES E
权利人:CORNELL RES FOUNDATION INC
摘要:Process for the stereoselective synthesis of 6β-and 8β- hydroxy epimers by the chemical reduction of 6- and 8-keto derivatives in the morphine and morphinan series utilizing alkaline formamidinesulficic acid. The 6β- and 8β-hydroxy derivatives obtained according to the invention evidence narcotic antagonist and/or agonist activity and are also useful in the chemical and pharmacological standardization of various morphine and codeine derivatives and metabolites.

专利号:US-4775759-A
优先权日:1984-11-27
标 题:Synthesis and utilization of 17-methyl and 17-cyclopropylmethyl-3,14-dihydroxy-4,5α-epoxy 6β-fluoromorphinans (foxy and cyclofoxy) as (18F)-labeled opioid ligands for position emission transaxial tomography (PETT)
发明人：RICE KENNER C; PERT CANDACE B; BURKE JR TERRENCE R; LARSON STEVEN M; ECKELMAN WILLIAM C; CHANNING MICHAEL A
权利人:US HEALTH
摘要:Fluorinated derivatives 3,14-dihydroxy-4,5α-epoxy-6β-fluoro-17-methylmorphinan ('fluorooxymorphone'; FOXY, compound 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5α-epoxy-6β-fluoromorphinan (CYCLOFOXY, compound 18) are prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11, respectively. Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6α-triflate functions in 8 and 16. The synthetic procedures were suitable for the production of the corresponding positron emitting 18 F-labeled analogs 18 F-FOXY and 18 F-CYCLOFOXY, which are useful for in vivo studies of the opioid receptor system using positron emission transaxial tomography. In addition, the tritiation of FOXY (10) to high specific activity is noted.

专利号:US-8227609-B2
优先权日:2005-02-11
标 题 :Process for purifying noroxymorphone compounds
发明人：WEIGL ULRICH; KOETZ ULF; FREIFELD ILIA
权利人:WEIGL ULRICH; KOETZ ULF; FREIFELD ILIA; CILAG AG
摘要:A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, α,β-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a selected noroxymorphone compound in a reaction which converts the hydroxyl groups present in the mixture to leaving groups of the formula —OR 2 in which R 2 is the introduced radical of the leaving group, (b) these leaving groups are optionally detached again, then (c) the resulting mixture is subjected to a selective hydrogenation, so that a saturated bond is formed in the α,β-position of the unsaturated noroxymorphone compounds and any remaining leaving groups are each converted to a hydroxyl group and then optionally (d) the pure noroxymorphone compound is isolated; processing of the noroxymorphone purified in this way to naltrexone or naloxone or a salt of these compounds or a quaternary derivative of these compounds; pharmaceutical formulations comprising such a compound.

专利号:US-10316042-B2
优先权日:2012-07-16
标题:Process for improved opioid synthesis
发明人：GEBBIE STUART JAMES; GIGUERE JOSHUA R; MCCARTHY KEITH; RIDER LONN S
权利人:RHODES TECH
摘要:Compounds and compositions for use as starting materials or intermediate materials in the preparation of opioids including, e.g., oxymorphone base and/or an oxymorphone salt; processes for preparing these compounds and compositions; uses of these compounds and compositions in the preparation of APIs and pharmaceutical dosage forms; and uses of said APIs and pharmaceutical dosage forms in the treatment of medical conditions.