CAS: 75507-68-5; Ethyl (2-Amino-6-((4-Fluorobenzyl)Amino)Pyridin-3-yl)Carbamate Maleate

上下游产品

2-amino-3-nitro-6-(p-fluoro-benzylamino)-pyridinep-fluorohippuric Acid

2-氨基-3-硝基-6-(4-氟苄基氨基)吡啶 在 氢气,三乙胺,Sodium Hydroxide,Palladium Dichloride体系中,用 水,乙酸乙酯,N,N-二甲基甲酰胺作为反应溶剂,70.0 °C,350.01 Kpa 条件下,反应 5.0H,获得 Flupirtine Maleate
参考文献:一种马来酸氟吡汀化合物的合成方法
标题:一种马来酸氟吡汀化合物的合成方法
摘要:本发明公开了一种马来酸氟吡汀化合物的合成方法,其使用2‑氨基‑3‑硝基‑6‑氯吡啶(化合物1)为起始原料,与对氟苄胺(化合物2)反应生成2‑氨基‑3‑硝基‑6‑对氟苄胺基吡啶(化合物3),经过二碳酸二叔丁酯保护得2‑氨基‑3‑硝基‑6‑对氟苄胺基吡啶‑3‑基‑乙酸叔丁酯(化合物4),经过氢化还原后与氯甲酸乙酯反应完毕,进行脱保护得到盐酸氟吡汀(化合物5),与马来酸成盐得马来酸氟吡汀(化合物6).该合成方法起始原料廉价易得,通过氨基保护避免副产物的生成,从而降低杂质含量,提高产品的质量,采用氯化钯进行催化还原,反应条件温和,反应过程易操作,适合工业化生产.

专利信息

专利号:US-5959115-A
优先权日:1997-04-23
标 题:Process for the preparation of pure flupirtine maleate and its A modification
发明人：OLBRICH ALFRED; EMIG PETER; KUTSCHER BERNHARD; LANDGRAF KARL-FRIEDRICH; PAULUHN SIEGFRIED; STANGE HANS
权利人:ASTA MEDICA AG
摘要:A process for preparation of pure flupertine maleate and the pure A crystalline form of flupertine maleate by the use of water soluble alcohols during synthesis and/or purification.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:CN-102241626-B
优先权日:2011-05-03
标题:Synthesis process of flupirtine maleate

专利号:CN-101208345-B
优先权日:2005-05-25
标 题 :(S) -N-methylnaltrexone, method of synthesis and pharmaceutical use thereof