CAS: 768-35-4; (3-Fluorophenyl)Boronic Acid

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CAS号1073-06-9 间溴氟苯 | CAS号625-98-9 间氯氟苯 | CAS号688-74-4 硼酸三丁酯 | CAS号17318-03-5 3-氟苯基溴化镁 | CAS号121-43-7 硼酸三甲酯 | CAS号402-67-5 间氟硝基苯 | CAS号350-46-9 对氟硝基苯 | CAS号372-20-3 3-氟苯酚 | CAS号396-64-5 3,3'-二氟联苯 | CAS号1496-00-0 1-Fluoro-3-benz... | CAS号914348-84-8 2-(3-氟苯基)噻唑-5-甲醛 | CAS号400751-05-5 3'-氟联苯-3-基胺 | CAS号2094-03-3 3-氟-联苯-2-羧酸 | CAS号5728-66-5 3'-氟-[1,1'-联苯]-4-胺 | CAS号54022-97-8 5-(3-氟苯基)呋喃-2-羧酸

(3-Fluorophenyl)-Dimethoxyborane置于盐酸体系中,用 水 作为反应溶剂,化学反应生成 3-氟苯基硼酸
参考文献:Mn 催化的芳烃 C-H 烯基化与末端炔烃
标题:Mn 催化的芳烃 C-H 烯基化与末端炔烃
摘要:描述了第一个锰催化的芳烃 Ch 烯基化与末端炔烃.该过程具有操作简单的催化剂系统,其中包含市售的 Mnbr(Co)(5) 和二环己胺 (Cy(2)Nh).该反应很容易以高度化学选择性,区域选择性和立体选择性的方式发生,以高产率提供抗马尔科夫尼科夫 E 构型的烯烃.实验研究和 Dft 计算表明 (1) 反应是由 Ch 活化步骤通过锰和碱的合作引发的;(2)锰环和炔基锰是反应的关键中间体;(3) 配体到配体的氢转移和炔基辅助的 Ch 活化是使反应在锰中具有催化作用的关键步骤.
DOI:10.1021/ja311689K

专利信息

专利号:US-7626045-B2
优先权日:2005-01-14
标题:Synthesis of himbacine analogs
发明人：THIRUVENGADAM TIRUVETTIPURAM K; WANG TAO; LIAO JING; CHIU JOHN S; TSAI DAVID J S; LEE HONG-CHANG; WU WENXUE; FU XIAOYONG
权利人:SCHERING CORP
摘要:The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. n An example of a step in the synthesis of such a himbacine analog is as follows:

专利号:EP-1853592-B1
优先权日:2005-01-14
标题:Synthesis of himbacine analogs
发明人：THIRUVENGADAM TIRUVETTIPURAM K; WANG TAO; LIAO JING; CHIU JOHN S; TSAI DAVID J S; LEE HONG-CHANG; WU WENXUE; FU XIAOYONG
权利人:SCHERING CORP
摘要:The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: Formula (I)

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

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:US-9732097-B2
优先权日:2015-05-11
标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor
发明人：ZHOU JIACHENG; QIAO LEI; WENG LINGKAI
权利人:INCYTE CORP
摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.