CAS: 143621-35-6; 2-((3-Aminopyridin-2-yl)Methylene)Hydrazine-1-Carbothioamide

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CAS号18699-87-1 2-甲基-3-硝基吡啶 | CAS号10261-94-6 3-硝基吡啶-2-甲醛 | CAS号79-19-6 硫代氨基脲 | CAS号116026-99-4 (2-甲酰基吡啶-3-基)氨基甲酸叔丁酯 | CAS号6298-19-7 2-氯-3-氨基吡啶 | CAS号5470-18-8 2-氯-3-硝基吡啶 | CAS号65156-92-5 N,N-dimethyl-2-...

📜N-2-Chloropyrid-3-Yl-Trimethylacetamide置于palladium Diacetate 盐酸,Sodium Acetate,臭氧,三苯基膦体系中,用 甲醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 24.33H,反应生成[(3-氨基吡啶-2-基)亚甲基氨基]硫脲
参考文献:3-氨基吡啶-2-羧醛硫半脲(3-Ap)的合成
标题:3-氨基吡啶-2-羧醛硫半脲(3-Ap)的合成
摘要:钯催化的甲基硼酸与2-氯-3-硝基吡啶的交叉偶联一步一步即可制得2-甲基-3-硝基吡啶4.用二氧化硒氧化4得到醛5.或者,将4与dmfdma缩合,然后氧化,以两步较高的收率获得5.随后将5与硫代氨基脲直接偶联,然后使用氯化亚锡或硫化钠还原硝基,得到3-Ap(3).用亚硫酸氢钠还原得到3-Hap(8).最后,设计了避免硝基功能降低的途径.因此,在heck反应条件下,苯乙烯与2-氯-3-氨基吡啶9的直接偶合得到16,该16转化为17,氧化为醛18并转化为3-Ap(3),并具有对t-Boc官能团的原位解封.
Doi:10.1016/s0040-4020(98)00328-7

专利信息

专利号:US-10189803-B2
优先权日:2008-02-22
标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
发明人：CHONG HYUN-SOON
权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH
摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-5869676-A
优先权日:1997-05-15
标题:Process for the synthesis of ribonucleotide reductase inhibitors 3-AP and 3-AMP
发明人：NIU CHUANSHENG; LI JUN; LI XIUYAN; DOYLE TERRENCE W; CHEN SHU-HUI
权利人:VION PHARMACEUTICALS INC
摘要:The present invention relates to improved, efficient chemical syntheses of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP).

专利号:US-8598153-B2
优先权日:2006-09-22
标题 :Method of treatment using fatty acid synthesis inhibitors
发明人：SINGH SHEO B; TOTA MICHAEL R; WANG JUN
权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME
摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.

专利号:US-2009298891-A1
优先权日:2005-09-16
标 题:Methods of Treating or Preventing Cancer Using Pyridine Carboxaldehyde Pyridine Thiosemicarbazone Radiosensitizing Agents
发明人：TOFILON PHILIP; CAMPHAUSEN KEVIN; GIUS DAVID
权利人:US GOV HEALTH & HUMAN SERV
摘要:The present invention features methods of inhibiting ribonucleotide reductase and DNA synthesis after administration of a dose of ionizing radiation to cells. The present invention further features methods of treating patients suffering from cancer comprising contemporaneous or sequential administration of a radiosensitizing dose of a 2-carboxyaldehyde pyridine thiosemicarbazone compound and ionizing radiation.