CAS: 877397-70-1; (R)-3-(1-(2,6-Dichloro-3-Fluorophenyl)Ethoxy)-2-Nitropyridine

上下游产品

3-hydroxy-2-nitropyridine (S)‐1‐(2,6-dichloro-3-fluorophenyl)ethanol (R)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol 3-fuoro-2-nitropyridine (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethyoxyl)-2-aminopyridine crizotinib 5-bromo-3-[1 (R)-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-pyridin-2-ylamine 4-(4-{6-amino-5-[(R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-pyridin-3-yl}-pyrazol-1-yl)-piperidine-1-carboxylic acid tert-butyl ester

1-(2,6-二氯-3-氟苯基)乙醇置于boc-L-脯氨酸,对甲苯磺酸,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,二氯甲烷 作为反应溶剂,化学反应 5.5H,反应生成 3-[[(1R)-1-(2,6-二氯-3-氟苯基)乙基]氧基]-2-硝基吡啶
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.

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.