6-碘吡啶-3-羧酸乙酯置于indium,水体系中,化学反应 10.0H,以64%的收率获得产物烟酸乙酯 参考文献:Dehalogenation And Barbier-Type Hydroxyalkylation Of π-Deficient Haloheterocycles Using Indium 标题:Dehalogenation And Barbier-Type Hydroxyalkylation Of π-Deficient Haloheterocycles Using Indium 摘要:The Reaction Of Pi-Deficient Haloheterocycles With Indium Metal In Water Gave Corresponding Dehalogenated Heterocycles. The Use Of Diluted Hydrochloric Acid Instead Of Water Accelerated The Reductive Reactivity Of Indium Metal. Furthermore,Barbier-Type Additions Proceeded By Reactions Of Alpha-Iodoheterocycles With Indium In The Presence Of Pivalaldehyde. DOI:10.3987/com-08-S(F)95
专利号:US-2024247022-A1 优先权日:2021-05-04 标 题 :A Process for Synthesis of Nicotinamide Riboside Chloride (NRCL) 发明人:MALKANNAGARI RAMANI; GUNDAPUNENI RAGHAVA RAO; BOHAN FRODE 权利人:BOHAN & CO AS 摘要:The present invention discloses synthesis of nicotinamide riboside chloride (NRCI). More particularly, the present invention describes cost effective and industrially scalable process for the synthesis of NRCI in amorphous form.
专利号:US-9567315-B1 优先权日:2016-04-22 标 题:Method for synthesis of 4-OH substituted anabaseine derivative 发明人:CHANG YU; HSU CHENG-FANG 权利人:INST NUCLEAR ENERGY RES ATOMIC ENERGY COUNCIL EXECUTIVE YUAN ROC 摘要:A method for synthesis of 4-OH substituted anabaseine derivative which is used as an α 7 receptor agonist is revealed. A nucleophilic substitution reaction of δ-valerolactam with ethyl nicotinate is carried out to get an intermediate product. Then heat the intermediate product under reflux with concentrated hydrochloric acid to get a cyclized product-anabaseine. Next anabaseine and 4-hydroxyethoxy-2-methoxybenzaldehyde are reacted under concentrated hydrochloric acid catalysis to get a 4-OH anabaseine derivative 3-[(4-Hydroxyethoxy-2-methoxy)-benzylidene]anabaseine. The 4-OH anabaseine derivative is synthesized and prepared easily by the present invention. Not only the steps for synthesis are simplified, the yield is as high as 60%. The product can be mass-produced.
专利号:US-8299206-B2 优先权日:2007-11-15 标题:Method of synthesis of morpholino oligomers 发明人:FOX CHRISTINA MARY JOSEPHINE; WELLER DWIGHT D 权利人:FOX CHRISTINA MARY JOSEPHINE; WELLER DWIGHT D; AVI BIOPHARMA INC 摘要:Improved methods are described for solid-phase synthesis of morpholino oligomers, in which a protected morpholino ring nitrogen is deprotected between coupling steps using a heterocyclic amine salt in a trifluoroethanol-containing solvent, where the salt is a salt of a heterocyclic amine, having a pKa in the range of 1-4 in its protonated form, with an acid selected from a sulfonic acid, trifluoroacetic acid, and hydrochloric acid. Examples are 3-chloropyridinium methanesulfonate (CPM) and 4-cyanopyridinium trifluoroacetate (CYTFA).
专利号:US-5530134-A 优先权日:1994-09-06 标 题 :Synthesis of anabaseine, salts and derivatives thereof 发明人:DANESHTALAB MOHSEN; NGUYEN DAI; SIDHU INDERJIT; MICETICH RONALD G 权利人:SYNPHAR LAB INC 摘要:A process for the synthesis of compounds of the formulas Ia and Ib below, wherein R 1 , R 2 , and R 3 , which are the same or different, are each selected from hydrogen and C 1 -C 4 alkyl, including the compound Anabaseine (Ia, wherein R 1 =R 2 R 3 =H) (3,4,5,6-tetrahydro-2', 3'-bipyridine), the process comprising reacting sodium salt of δ-valerolactone with substituted ethyl nicotinate derivative to produce the Claisen product sodium 3-nicotinoyl-2-tetrahydropyranone enolate derivative, heating the sodium 3-nicotinoyl-2-tetrahydropyranone enolate derivative with concentrated HCl to produce 3-(5-chloro-1-pentanone-1-yl) pyridine derivative, dissolving the 3-(5-chloro-1-pentanone-1-yl) pyridine derivative in ethanol and then heating the 3-(5-chloro-1-pentanone-1-yl) pyridine derivative in ethanol with ethanolic ammonia solution in a sealed container to produce the compound Ia. Also, the process steps in the above process, and the products and intermediate products produced thereby. ##STR1##
专利号:US-6951878-B2 优先权日:1998-03-12 标 题:Benzo[b]thiophenyl or tetrahydro-benzo[b]thiophenyl modulators of protein tyrosine phosphatases (PTPases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILLIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
[参考文献]: Adel S Girgis, Et Al. Synthesis Of New 3-Pyridinecarboxylates Of Potential Vasodilation Properties. Eur J Med Chem. 2008 Sep;43(9):1818-27. [参考文献]: C M Mills, Et Al. Transdermal Nicotine Suppresses Cutaneous Inflammation. Arch Dermatol. 1997 Jul;133(7):823-5. [参考文献]: K Sugibayashi, Et Al. Simultaneous Transport And Metabolism Of Ethyl Nicotinate In Hairless Rat Skin After Its Topical Application: The Effect Of Enzyme Distribution In Skin. J Control Release. 1999 Nov 1;62(1-2):201-8. [参考文献]: Kenji Sugibayashi, Et Al. Utility Of A Three-Dimensional Cultured Human Skin Model As A Tool To Evaluate The Simultaneous Diffusion And Metabolism Of Ethyl Nicotinate In Skin. Drug Metab Pharmacokinet. 2004 Oct;19(5):352-62. [参考文献]: M Sakamoto, Et Al. Inhibitory Effects Of Niacin And Its Analogues On Induction Of Ornithine Decarboxylase Activity By Diethylnitrosamine In Rat Liver. Biochem Pharmacol. 1987 Sep 15;36(18):3015-9.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 319. 摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2014) 4, 171. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 198. 摘要:Davies, H. M. L.; Morton, D., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 537. 摘要:Davies, H. M. L.; Morton, D., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 533.