CAS: 23277-43-2; Nalbuphine Hydrochloride

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CAS号20594-83-6 纳布啡 | CAS号16676-33-8 6-Keto Nalbuphine

📜14-羟基二氢降吗啡酮盐酸盐置于盐酸,Potassium Tri-Sec-Butyl-Borohydride,溶剂黄146,Tetramethylammonium Triacetoxyborohydride体系中,用 四氢呋喃,水,二甲基亚砜,N,N-二甲基甲酰胺 用作溶剂,化学反应生成纳布啡盐酸盐水合物
参考文献:One-Pot Process For Synthesis Of Nalbuphine Hydrochloride And Impurity Control Strategy
标题:One-Pot Process For Synthesis Of Nalbuphine Hydrochloride And Impurity Control Strategy
摘要:An Improved Kilogram-Scale Process Of Synthesis Of Nalbuphine Was Developed By Investigating The Critical Parameters. Ten Process-Related Impurities Were Identified,Of Which The Source And Control Strategy Was Elucidated. Moreover,Tetramethylammonium Triacetoxyborohydride (Me4Nbh(Oac)(3)) Was Developed To Reduce The Imine And Ketone In One Pot. As A Result,6-Beta-Epimer Was Significantly Controlled To Only 0.08% In The Crude Nalbuphine. The Improved Process Was Robust At Kilogram Scale In 60.4% Overall Yield With 99.95% High-Performance Liquid Chromatography (HPLC) Purity.
Doi:10.1021/acs.Oprd.0C00321

专利信息

专利号:US-5756745-A
优先权日:1994-05-31
标题 :Preparation of nalbuphine having low levels of β-epimer
发明人：KAVKA FRANK
权利人:MALLINCKRODT MEDICAL INC
摘要:A process is described for the synthesis of nalbuphine. The process results in a product having very low levels of the undesirable β-epimer. The process is a five-step synthesis that begins with a compound such as an N,O 3 -bis (alkoxycarbonyl) -14-hydroxynormorphinone.

专利号:US-2013030282-A1
优先权日:2011-07-18
标题:Synthesis and characterization of near ir fluorescent magnetic and non-magnetic albumin nanoparticles for biomedical applications
发明人：MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL
权利人:UNIV BAR ILAN; MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL
摘要:The present invention discloses Near Infrared (NIR) fluorescent albumin nanoparticles having a structure selected from a core structure or a core-shell structure. Also disclosed are a process of preparing these NIR fluorescent albumin nanoparticles, and a method of in vivo detection of pathologies, in particular cancer pathology, by using administering these NIR fluorescent albumin nanoparticles to a patient.

专利号:US-2004138238-A1
优先权日:2002-08-08
标题 :Substituted aminopyrimidine compounds as neurokinin antagonists
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY
摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

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:CN-110330500-B
优先权日:2019-07-12
标 题 :A kind of stereoselective synthesis method of 6β-hydroxy-7,8-dihydro-morphine derivatives

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 %.