2-Hydroxyimino-3-Oxo-3-(4-Pyridyl)-Propanoic Acid Ethyl Ester置于盐酸,乙醇,钯,铂,Tin(Ll) Chloride体系中,化学反应 2.0H,反应生成4-(2-氨基乙基)吡啶 参考文献:Amines Related To Epinephrine. V. Pyridine Compounds Analogous To Epinephrine,Adrenalene And Ephedrine 标题:Amines Related To Epinephrine. V. Pyridine Compounds Analogous To Epinephrine,Adrenalene And Ephedrine 摘要: Doi:10.1021/ja01225A017
专利号:US-3933830-A 优先权日:1974-09-10 标 题 :Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines 发明人:BARTH WAYNE E; KUHLA DONALD E 权利人:PFIZER 摘要:Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structure ##EQU1## wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms. n Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structure ##EQU2## with substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art. n The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.
专利号:WO-2017082924-A1 优先权日:2015-11-13 标题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE TERRENCE R JR; HYMEL DAVID 权利人:THE US SECRETARY DEPT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:WO-2023081730-A1 优先权日:2021-11-03 标 题:4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid cb2 receptor modulators for the treatment of cancer 发明人:ELZEIN ELFATIH; LIU JIWEN 权利人:TEON THERAPEUTICS INC 摘要:The present invention relates to 82 specific 4-hydroxy-2-oxo-1,2- dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid CB2 receptor modulators for the treatment of cancer, e.g. to 6-(4- fluorophenyl)-4-hydroxy-1-(2-(4-methylpiperazin-1-yl)ethyl)-2-oxo-N- (spiro[2.3]hexan-5-yl)-1,2-dihydro-1,8-naphthyridine-3-carboxamide (example 1, compound 1) The present description discloses the synthesis and characterisation of the 82 claimed compounds as well as biological assays thereof.
专利号:US-3992388-A 优先权日:1974-09-10 标题 :4-(2-Pyridylamidoethyl)piperidines 发明人:BARTH WAYNE E; KUHLA DONALD E 权利人:PFIZER 摘要:Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structue ##SPC1## n Wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms. n Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structue ##SPC2## n With substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art. n The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.
专利号:US-2009227575-A1 优先权日:2008-03-04 标 题 :7H-PYRROLO[2,3-H]QUINAZOLINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS 发明人:VENKATESAN ARANAPAKAM MUDUMBAI; CHEN ZECHENG; DOS SANTOS OSVALDO; BROOIJMANS NATASJA; GOPALSAMY ARIAMALA 权利人:WYETH CORP 摘要:A 7H-pyrrolo[2,3-h]quinazoline compound of the formula I n n n n n n n n n n wherein Ar, R 1 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and n are as defined in the specification, and methods for making same.
[参考文献]: Willem M Albers, Et Al. Self-Assembly Of Pyridine-Modified Lipoic Acid Derivatives On Gold And Their Interaction With Thyroxine (T4). Int J Mol Sci. 2013 Feb 6;14(2):3500-13.
合成参考文献
参考文献:10.1007/978-1-61779-148-2_6 摘要:Krusemark CJ, Frey BL, Smith LM, Belshaw PJ. Complete chemical modification of amine and acid functional groups of peptides and small proteins. Methods Mol Biol. 2011;753():77–91.