2-乙烯基吡啶置于氯化铵体系中,用 甲醇,水 用作溶剂,化学反应 16.0H,以29%的收率获得2-(2-氨乙基)吡啶 参考文献:Modification And Optimization Of The Bis-Picolylamide-Based Relay Protection For Carboxylic Acids To Be Cleaved By Unusual Complexation With Cu2+ Salts 标题:Modification And Optimization Of The Bis-Picolylamide-Based Relay Protection For Carboxylic Acids To Be Cleaved By Unusual Complexation With Cu2+ Salts 摘要:A Simple Modification Of Our Recently Published Protection Scheme For Carboxylic Acids As Amides Resulted In A New Protecting Group With Significantly Improved Properties. It Requires Shorter Reaction Times For Deprotection And Allows Us To Replace Cu(Otf)(2) By Cucl2,Indicating At The Same Time The Importance Of The Nature Of The Anion Of The Cu2+ Source. Since The New Scheme Fulfills All Criteria Required For An Ideal Protection Group It Should Find Widespread Application In Synthetic Organic Chemistry. Doi:10.1021/jo301349T
专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-2002103381-A1 优先权日:2000-11-30 标 题 :Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.
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:US-6569834-B1 优先权日:1992-12-03 标 题 :Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides 发明人:PETTIT GEORGE R; BARKOCZY JOZSEF 摘要:Dolastatin 10, a linear pentapeptide, has shown potent antineoplastic activity profiles against various experimental cancer systems. The synthesis of structural modifications of dolastatin 10 having significant antineoplastic activity against human cancer cell lines has been accomplished; namely antineoplastic tetrapeptide w-amino alkyl amides related to dolastatin 10, which have been found to demonstrate effective antineoplastic activity against various human cancer cell lines. Members of this have demonstrated significant antineoplastic activity against human cancer cell lines. The human cancer cell lines against which the substances of the present invention have yielded the significant antineoplastic activity are: Ovarian OVCAR-3; Central Nervous System ('CNS') SF295; Renal A498; Lung NCI460; Colon KM20L2 and Melanoma SK-MEL-3.
专利号:WO-2004020401-A1 优先权日:2002-09-02 标题 :Synthesis of sulfonamide derivatives 发明人:KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM 权利人:SYNGENE INTERNAT PRIVATE LTD; KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM 摘要:The novel method of synthesis of sulphonamide derivatives (I), comprising reaction of alkyl-4-halophenylsulfonate with an amine. Formula (I) wherein X is halogen and R1 and R2 are independently selected from group comprising (i) C1 to C15 alkyl, straight or branched, (ii) C3 to C15 cycloalkyl, substituted or unsubstituted, (iii) C2 to C15 alkenyl, straight or branched, (iv) C2 to C15 alkynyl, straight or branched, (v) phenyl or benzyl, substituted or unsubstituted, (vi) heterocycloalkyl, substituted or unsubstituted, (vii) hydrogen, (viii) form with the nitrogen to which they are attached a 3-7 membered heterocyclic moiety such as pyrolidine, piperidine, piperazine, imidazole, pyrazole, (ix) the alkyl in i) may be attached to a moiety selected from cycloalkyl or heterocycloalkyl, substituted or unsubstituted
专利号:US-2024425446-A1 优先权日:2023-06-23 标题:Dichloromethane-free synthesis of cyclopropenimines 发明人:HEDRICK JAMES L; CAMPOS LUIS M; PARK NATHANIEL H; WU DINO 权利人:IBM; THE TRUSTEE OF COLUMBIA UNIV IN THE CITY OF NEW YORK 摘要:A process of forming a cyclopropenimine (CPI) is disclosed. The process includes obtaining a solution of pentachlorocyclopropane (PCC) dissolved in a first solvent and adding a secondary amine to the solution. The process further includes obtaining precipitated products, including a CPI chloride (CPI−Cl) salt and a secondary amine salt, of a reaction between the secondary amine and the PCC and mixing the precipitated products in a second solvent. The CPI−Cl salt is substantially soluble in the second solvent and the secondary amine salt is substantially insoluble in the second solvent. A CPI composition, an apparatus containing the CPI composition, a process of capturing carbon dioxide (CO2) with the CPI composition, and a process of generating carbonate with the CPI composition are also disclosed.
[参考文献]: Alessio Innocenti, Et Al. Carbonic Anhydrase Activators. Activation Of The Membrane-Associated Isoform Xv With Amino Acids And Amines. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3430-3. [参考文献]: Alessio Innocenti, Et Al. Carbonic Anhydrase Activators: Activation Of The Archaeal Beta-Class (Cab) And Gamma-Class (Cam) Carbonic Anhydrases With Amino Acids And Amines. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6194-8. [参考文献]: Anthony Bertucci, Et Al. Carbonic Anhydrase Activators. The First Activation Study Of A Coral Secretory Isoform With Amino Acids And Amines. Bioorg Med Chem. 2010 Mar 15;18(6):2300-2303. [参考文献]: Daniela Vullo, Et Al. Carbonic Anhydrase Activators: Activation Of The Human Cytosolic Isozyme Iii And Membrane-Associated Isoform Iv With Amino Acids And Amines. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4303-7. [参考文献]: Daniela Vullo, Et Al. Carbonic Anhydrase Activators: Activation Of The Human Isoforms Vii (Cytosolic) And Xiv (Transmembrane) With Amino Acids And Amines. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4107-12.
合成参考文献
参考文献:10.1107/s1600536811009809 摘要:Chiririwa H, Moss JR, Su H, Hendricks D, Meijboom R. 1,4-Bis[(2-pyridyl-eth-yl)imino-meth-yl]benzene. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o921. 参考文献:10.1021/ic200409d 摘要:Majumder S, Sarkar S, Sasmal S, Sañudo EC, Mohanta S. Heterobridged dinuclear, tetranuclear, dinuclear-based 1-d, and heptanuclear-based 1-D complexes of copper(II) derived from a dinucleating ligand: syntheses, structures, magnetochemistry, spectroscopy, and catecholase activity. Inorg Chem. 2011 Aug 15;50(16):7540–54. doi: 10.1021/ic200409d.