6-氨基烟酸甲酯置于lithium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应生成 6-氨基烟酸 参考文献: Histone Deacetylase Inhibitors For Immunomodulation In Tumor Microenvironment[fr] Inhibiteurs D'Histone Désacétylase Pour L'Immuno-Modulation Dans Un Micro-Environnement Tumoral 标题: Histone Deacetylase Inhibitors For Immunomodulation In Tumor Microenvironment[fr] Inhibiteurs D'Histone Désacétylase Pour L'Immuno-Modulation Dans Un Micro-Environnement Tumoral 摘要:提供的是类i Hdac抑制剂化合物,它们的生产和应用.这些化合物在肿瘤微环境(tme)中具有表观遗传免疫调节活性,从而抑制肿瘤细胞的生长.
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-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
专利号:US-4375545-A 优先权日:1981-06-22 标 题 :Process for the synthesis of the nicotinyl ester of 6-aminonicotinic acid 发明人:WARNER JR PAUL L; LUBER JR EDWARD J; SOMERVILLE WILLIAM A; ZUSI F CHRISTOPHER 权利人:WESTWOOD PHARMACEUTICALS INC 摘要:6-Aminonicotinic acid is reacted with an alkali carbonate selected from the group consisting of sodium carbonate and potassium carbonate. The reaction is carried out at elevated temperature and in dimethylformamide. The 6-aminonicotinic acid alkali salt so produced is reacted with 3-chloromethylpyridine hydrochloride. The reaction is carried out at elevated temperature and in dimethylformamide. The desired nicotinyl ester is thus produced.
专利号:US-11702652-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries
专利号:US-2009264300-A1 优先权日:2005-12-01 标题 :Enzymatic encoding methods for efficient synthesis of large libraries
专利号:US-5169935-A 优先权日:1990-06-20 标 题:Method of making peptides 发明人:HOEGER CARL A; THEOBALD PAULA G; PORTER JOHN S; RIVIER JEAN E F 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:Methods for making peptides of a suitable length for solid phase synthesis, which peptides include in their sequence a pair of residues of a different character which have acylated side chains and a residue which has an N-alkylated side chain. A peptide intermediate is constructed on the resin using commercially available starting materials. The N-terminus can be acylated by removing the alpha -amino protecting group and acylating under standard conditions. First primary amino protecting groups included in those residues to be acylated are removed, and acylation is effected, preferably by using a carboxypyridine or a similar heterocyclic acylating agent. Following such side chain acylation, a second protecting group included in the residue to be N-alkylated is removed, and the N-alkylation reaction is carried out while the peptide remains on the resin using a borohydride and an appropriate aldehyde or ketone. Following cleavage from the resin and removal of any protecting groups still remaining, the peptide is appropriately purified, thus requiring only a single purification to be carried out while forming a synthetic peptide including residues for which the modified amino acids are not readily commercially available.
[参考文献]: Petersen Jg, Et Al. Synthesis And Pharmacological Evaluation Of 6-Aminonicotinic Acid Analogues As Novel Gaba(A) Receptor Agonists. Eur J Med Chem. 2014 Sep 12;84:404-16. [参考文献]: D J Jamieson, Et Al. Two Genetically Distinct Pathways For Transcriptional Regulation Of Anaerobic Gene Expression In Salmonella Typhimurium. J Bacteriol. 1986 Oct;168(1):389-97.
合成参考文献
参考文献:10.1007/s11030-008-9072-1 摘要:Hulme C, Lee YS. Emerging approaches for the syntheses of bicyclic imidazo[1,2-x]-heterocycles. Mol Divers. 2008 Feb;12(1):1–15. doi: 10.1007/s11030-008-9072-1. 摘要:Spitzner, D., Science of Synthesis, (2005) 15, 194.