CAS: 290835-85-7; 2',6'-Dichloro-3'-Fluoroacetophenone

上下游产品

1-(2,6-二氯-3-氟苯基)乙醇 1-(2,6-Dichloro-3-Fluorophenyl)Ethanol 756520-66-8
(S)-1-(2,6-二氯-3-氟苯基)乙醇 (S)-1-(2,6-Dichloro-3-Fluorophenyl)Ethan-1-Ol 877397-65-4

1-(2,6-二氯-3-氟苯基)乙醇置于chloroamine-T,Zinc Dibromide体系中,用 乙腈 用作溶剂,化学反应 5.0H,以93%的收率获得2,6-二氯-3-氟苯乙酮
参考文献:锌(II)用氯胺-T催化醇氧化为羰基化合物
标题:锌(II)用氯胺-T催化醇氧化为羰基化合物
摘要:伯醇和仲醇有效氧化为相应的羰基化合物可以在乙腈中使用氯胺-T在催化锌(II)盐存在下进行.在没有羧酸副产物的情况下,伯醇被选择性地氧化为醛.
Doi:10.1016/j.Tetlet.2012.11.076

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:CN-112125841-A
优先权日:2020-10-23
标题:A new method for the synthesis of crizotinib intermediates

专利号:CN-119662581-A
优先权日:2025-01-27
标题 :Carbonyl reductase BsCR mutant, engineered bacteria and application in the synthesis of crizotinib chiral intermediates

专利号:US-2013072495-A1
优先权日:2010-05-14
标 题 :Fused bicyclic kinase inhibitors
发明人：LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G
权利人:LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.