CAS: 168823-76-5; 5-Bromo-2-(Chloromethyl)Pyridine

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CAS号88139-91-7 5-溴-2-吡啶甲醇 | CAS号900186-88-1 (5-Bromo-2-pyri... | CAS号31181-90-5 5-溴吡啶-2-甲醛 | CAS号3430-13-5 5-溴-2-甲基吡啶 | CAS号31181-64-3 2-甲基-5-溴吡啶 N-氧化物 | CAS号29682-15-3 5-溴吡啶-2-羧酸甲酯 | CAS号380893-73-2 (5-溴吡啶-2-基)甲基磷酸二乙酯

📜2-甲基-5-溴吡啶-N-氧化物置于氯化亚砜,乙酸酐体系中,用 二氯甲烷 用作溶剂,化学反应 12.0H,反应生成5-溴-2-(氯甲基)吡啶
参考文献:Inhibition Of 1-Deoxy-D-Xylulose-5-Phosphate Reductoisomerase By Lipophilic Phosphonates: Sar,Qsar,And Crystallographic Studies
标题:Inhibition Of 1-Deoxy-D-Xylulose-5-Phosphate Reductoisomerase By Lipophilic Phosphonates: Sar,Qsar,And Crystallographic Studies
摘要:1-Deoxy-D-Xylulose-5-Phosphate Reductoisomerase (Dxr) Is A Novel Target For Developing New Antibacterial (Including Antituberculosis) And Antimalaria Drugs. Forty-One Lipophilic Phosphonates,Representing A New Class Of Dxr Inhibitors,Were Synthesized,Among Which 5-Phenylpyridin-2-Ylmethylphosphonic Acid Possesses The Most Activity Against E. Coli Dxr (Ecdxr) With A K-I Of 420 Nm. Structure-Activity Relationships (Sar) Are Discussed,Which Can Be Rationalized Using Our Ecdxr:Inhibitor Structures,And A Predictive Quantitative Sar (Qsar) Model Is Also Developed. Since Inhibition Studies Of Dxr From Mycobacterium Tuberculosis (Mtdxr) Have Not Been Performed Well,48 Ecdxr Inhibitors With A Broad Chemical Diversity Were Found,However,To Generally Exhibit Considerably Reduced Activity Against Mtdxr. The Crystal Structure Of A,Mtdxr:Inhibitor Complex Reveals The Flexible Loop Containing The Residues 198-208 Has No Strong Interactions With The 3,4-Dichlorophenyl Group Of The Inhibitor,Representing A Structural Basis For The Reduced Activity. Overall,These Results Provide Implications In The Future Design And Development Of Potent Dxr Inhibitors.
Doi:10.1021/jm200363D

专利信息

专利号:US-8329905-B2
优先权日:2006-06-30
标 题 :Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
发明人：YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K
权利人:YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K; MERCK SHARP & DOHME
摘要:This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: n nwherein R 9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R 11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X 2 is Cl, Br, or I; X 3 is selected from Cl and Br; and PdL n is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.

专利号:US-8618314-B2
优先权日:2005-01-14
标 题 :Exo- and diastereo-selective synthesis of himbacine analogs
发明人：WU GEORGE G; SUDHAKAR ANANTHA; WANG TAO; XIE JI; CHEN FRANK X; POIRIER MARC; HUANG MINGSHENG; SABESAN VIJAY; KWOK DAW-LONG; CUI JIAN; YANG XIAOJING; THIRUVENGADAM TIRUVETTIPURAM K; LIAO JING; ZAVIALOV ILIA; NGUYEN HOA N; LIM NGIAP KIE
权利人:WU GEORGE G; SUDHAKAR ANANTHA; WANG TAO; XIE JI; CHEN FRANK X; POIRIER MARC; HUANG MINGSHENG; SABESAN VIJAY; KWOK DAW-LONG; CUI JIAN; YANG XIAOJING; THIRUVENGADAM TIRUVETTIPURAM K; LIAO JING; ZAVIALOV ILIA; NGUYEN HOA N; LIM NGIAP KIE; MERCK SHARP & DOHME
摘要:This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:

专利号:EP-2046804-B1
优先权日:2006-06-30
标题 :Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2-yl]methyl} phosphonate used in the synthesis of himbacine analogs

专利号:WO-2008005348-A1
优先权日:2006-06-30
标 题:Synthesis of diethyl{ i5' (3 -fluorophenyl) -pyridine-2-yl] methyl} phosphonate used in the synthesis of himbacine analogs

专利号:US-2008004449-A1
优先权日:2006-06-30
标题:Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate

专利号:US-8258319-B2
优先权日:2005-01-14
标 题:Exo- and diastereo- selective synthesis of himbacine analogs