CAS: 38186-88-8; 2-Chloro-5-Fluoronicotinic Acid

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CAS号82671-06-5 2,6-二氯-5-氟烟酸 | CAS号139911-30-1 2-氯-5-氟烟酸乙酯 | CAS号1316084-72-6 (2E,4Z)-ethyl 2... | CAS号791644-48-9 2-氯-5-氟烟腈 | CAS号884495-37-8 2-氯-3-氨基-5-氟吡啶 | CAS号884494-33-1 2-氯-5-氟-3-碘吡啶 | CAS号847729-27-5 2-氯-5-氟烟酸甲酯 | CAS号1034667-22-5 5-氟-1H-吡唑并[3,4-... | CAS号139911-30-1 2-氯-5-氟烟酸乙酯 | CAS号1256822-80-6 3-溴-5-氟-1H-吡唑并[... | CAS号1196154-03-6 2-氨基-5-氟烟酸 | CAS号75302-64-6 2-氯-5-氟烟酰胺 | CAS号919294-92-1 2-(3,4-difluoro...

2,6-二氯-5-氟烟酸置于palladium Diacetate 甲酸,三乙胺,三苯基膦体系中,用 N,N-二甲基乙酰胺 用作溶剂,化学反应 7.0H,以70%的收率获得2-氯-5-氟烟酸
参考文献:实用合成2-((1 H-吡咯并[2,3-B]吡啶-4-基)甲氨基)-5-氟烟酸
标题:实用合成2-((1 H-吡咯并[2,3-B]吡啶-4-基)甲氨基)-5-氟烟酸
摘要:描述了关键药物中间体2-[((1 H-吡咯并[2,3-B]吡啶-4-基)甲基氨基]-5-氟烟酸(1))的实用合成.为了经由钯催化的氰化/还原序列引入2的氨基甲基部分,开发了经由n-氧化物的7-氮杂吲哚的区域选择性氯化.发现2,6-二氯-5-氟烟酸的高度选择性单脱氯可提供烟酸3.然后将两个构件2和3耦合以完成1的准备.
Doi:10.1021/jo0602571

专利信息

专利号:US-8598361-B2
优先权日:2007-07-31
标题 :Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives therof
发明人：JIMENEZ JUAN-MIGUEL; MILLER ANDREW; COLLIER PHILIP; GREEN JEREMY; DROS ALBERT; GAO HUAI; HAMON SYLVAIN
权利人:JIMENEZ JUAN-MIGUEL; MILLER ANDREW; COLLIER PHILIP; GREEN JEREMY; DROS ALBERT; GAO HUAI; HAMON SYLVAIN; VERTEX PHARMA
摘要:The present invention relates to a process for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or derivatives thereof.

专利号:US-2013211090-A1
优先权日:2010-09-03
标题:Method for the production of 5-fluoro-1h-pyrazolo[3,4-b]pyridine-3-carbonitrile
发明人：FOLLMANN MARKUS; ACKERSTAFF JENS
权利人:FOLLMANN MARKUS; ACKERSTAFF JENS; BAYER IP GMBH
摘要:The present invention relates to a process for preparing 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile of the formula (I) n n n n n n n n n n which serves as a synthesis intermediate for production of medicaments, especially for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

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优先权日:2021-07-15
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优先权日:2022-05-17
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