CAS: 877397-71-2; (R)-3-(1-(2,6-Dichloro-3-Fluorophenyl)Ethoxy)Pyridin-2-Amine

该化合物是一种手性小分子化合物,其基芯为矿物质组所替代的丙烯基和2,6-二氯-3-氟苯基杂音,其立体特性(R)配置增强了生物化学相互作用的选择性,使其对药物研究,特别是动脉抑制研究具有价值.卤素替代成分(氯和氟)的存在有助于目标接触的稳定性和结合性.该化合物通常被用作生物活性分子合成的中间体,为药物发现应用提供精确的结构控制.其定义明确的化学特性和高纯度使其适合机械研究和结构-活动关系调查.

结构式图片

相似化合物

877397-70-1 877399-00-3 877399-00-3

物理性质

MSDS等安全信息

上下游产品

(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethyoxyl)-2-nitropyridine (S)‐1‐(2,6-dichloro-3-fluorophenyl)ethanol 3-hydroxy-2-nitropyridine (R)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol (R)-tert-butyl 5-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)isoindoline-2-carboxylate (R)-5-(2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-7-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1,2,3,4-tetrahydroisoquinoline-7-yl)pyridin-2-amine (R)-5-(2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine

合成工艺路线路线简述

  • 877397-70-1 = 877397-71-2
    反应条件:1.1 Reagents: Carbon,Iron Chloride (Fecl3) Solvents: Ethanol; Rt -> 60 °C1.2 Reagents: Hydrazine Hydrate (1:1); 60 °C; 1 H,60 °C
    标题:Improved Synthesis Of Crizotinib
    作者:Zhang,Guang-Yan; Li,Peng-Cheng; Liu,Di-Fa; Guan,Jing-Xin; Gong,Ping; Et Al
    参考文献:Zhongguo Yaowu Huaxue Zazhi 日期:2014 卷标:24(6) 页码:445-449]

    877397-70-1 = 877397-71-2
    反应条件:1.1 Reagents: Hydrogen Solvents: Dichloromethane; 30 Psi,25 °C
    标题:Synthesis Of A Crizotinib Intermediate Via Highly Efficient Catalytic Hydrogenation In Continuous Flow
    作者:Xu,Feng; Chen,Jianli; Xie,Xiaoxuan; Cheng,Pengfei; Yu,Zhiqun; Et Al
    参考文献:Organic Process Research & Development 日期:2020 卷标:24(10) 页码:2252-2259
📜1-(2,6-二氯-3-氟苯基)乙醇置于boc-L-脯氨酸,铁粉,对甲苯磺酸,溶剂黄146,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三苯基膦,偶氮二甲酸二乙酯体系中,用 四氢呋喃,乙醇,二氯甲烷 作为反应溶剂,化学反应 6.0H,反应生成 (R)-3-(1-(2,6-二氯-3-氟苯基)乙氧基)吡啶-2-胺
参考文献:一种抗肿瘤分子靶向药物克里唑替尼的合成工 艺方法
标题:一种抗肿瘤分子靶向药物克里唑替尼的合成工 艺方法
摘要:本发明为一种新的抗肿瘤分子靶向药物克里唑替尼的合成工艺方法,涉及克里唑替尼前体的手性异构体的拆分工艺优化和副产物回收利用.本发明采用boc-L-脯氨酸(n-叔丁氧基羰基-L-脯氨酸)与催化剂对甲苯磺酸和缩合剂1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐相组合的催化拆分方法,将1-(2,6-二氯-3-氟代苯基)乙醇消旋体拆分为s-型醇和r-型醇,将拆分副产物混合物水解,并进行构型转换,制得s型醇1-(2,6-二氯-3-氟代苯基)乙醇,使其总收率由30%提高到了76%,而且缩短了时间,减少了污染,易于实施工业化生产.

海关参考信息

专利信息


专利号:US-7465842-B2
优先权日:2004-08-26
标 题 :Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
发明人：KUNG PEI-PEI; MARTINEZ CARLOS; TAO JUNHUA
权利人:AGOURON PHARMA
摘要:The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral (S)-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.

专利号:US-8785632-B2
优先权日:2004-08-26
标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
发明人：CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE
权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER
摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

专利号:US-2006178374-A1
优先权日:2004-08-26
标 题 :Aminoheteroaryl compounds as protein kinase inhibitors
发明人：CUI JINGRONG J; FUNK LEE A; JIA LEI; KUNG PEI-PEI; MENG JERRY J; NAMBU MITCHELL D; PAIRISH MASON A; SHEN HONG; TRAN-DUBE MICHELLE
权利人:AGOURON PHARMA
摘要:Aminoheteroaryl compounds are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

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合成参考文献


摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2014).
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