CAS: 330156-50-8; (R)-1-(2,6-Dichloro-3-Fluorophenyl)Ethanol

上下游产品

CAS号877397-67-6 1-(2,6-dichloro... | CAS号756520-66-8 1-(2,6-二氯-3-氟苯基)乙醇 | CAS号877397-65-4 (s)-1-(2,6-二氯-3... | CAS号1365267-27-1 恩沙替尼(X-376) | CAS号877397-70-1 (R)-3-(1-(2,6-二...

2,6-二氯-3-氟苯乙酮置于三乙氧基硅烷体系中,用 四氢呋喃,叔丁醇 用作溶剂,化学反应 12.0H,以86.7%的收率获得(R)-1-(2,6-二氯-3-氟苯基)乙醇
参考文献:一种克唑替尼的合成方法及其中间体制备方 法
标题:一种克唑替尼的合成方法及其中间体制备方 法
摘要:本发明提供了一种克唑替尼的合成方法及其中间体制备方法.本发明是以n‑保护的4‑(3‑(5‑氟‑6‑硝基吡啶‑3‑基)‑1H‑吡唑‑1‑基)哌啶(9)为原料,将其与手性中间体(3)进行反应,得到关键手性中间体,手性中间体再经还原,脱保护得到目标化合物克唑替尼(1).本发明的原料易得,反应条件温和,操作简便,催化剂具有非常好的稳定性和活性,易于回收和套用,便于克唑替尼大规模制备和生产.

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:WO-2019100785-A1
优先权日:2017-11-23
标题 :Synthesis process for crizotinib intermediate
发明人：XU LIANG; MAO BO; LI YANXIONG
权利人:ZHONGSHAN ENANTIOTECH CORPORATION LTD
摘要:Disclosed in the present invention is a synthesis process for a crizotinib intermediate. The synthesis process comprises the following steps: in an alkali and solvent environment, with 2,6-dichloro-3-fluoroacetophenone as a raw material and hydrogen as a reducing agent, reacting under the action of a chiral catalyst to obtain (R)-1-(2,6-dichloro-3-fluorophenyl)ethyl alcohol. A crizotinib chiral intermediate with high chiral purity is obtained at one step as the process uses the reduction system, complex chiral resolution procedures of the existing process are omitted, the period of the process is greatly shortened, production costs are low, reaction conditions are mild, the process is stable, the conversion rate is high, the environment pollution caused by the reaction is small, and the synthesis process is favorable for realizing the industrial production.

专利号:CN-108285908-B
优先权日:2017-12-26
标题 :A kind of method for immobilized double enzyme catalyzed synthesis of (S)-1-(2,6-dichloro-3-fluoro-phenyl)ethanol

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.

专利号:CN-107365301-B
优先权日:2016-05-12
标 题:Synthesis method of crizotinib and preparation method of intermediate thereof