Potassium Trifluoro(2-Fluoro-4-Methoxyphenyl)Boranuide置于lithium Hydroxide Monohydrate,Silver Trifluoromethanesulfonate,Selectfluor体系中,用 乙酸乙酯 用作溶剂,以77%的收率获得3,4-二氟苯甲醚 参考文献:Silver-Mediated Fluorination Of Potassium Aryltrifluoroborates With Selectfluor® 标题:Silver-Mediated Fluorination Of Potassium Aryltrifluoroborates With Selectfluor® 摘要:A Simple And Practical Procedure For The Silver-Mediated Fluorination Of Aryl-And Heteroaryltrifluoroborates With Electrophilic Fluorine From Selectfluor (R) And Lioh Center Dot H2O Is Presented. The Reaction Procedure Is Simple And Easy To Set Up,The Process Produces Fluorinated Arenes And Heteroarenes In Good To Excellent Yields And A Wide Range Of Electronically And Structurally Diverse Substrates Are Tolerated. (C) 2014 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tet.2014.10.055
专利号:US-10995078-B2 优先权日:2013-03-13 标 题:Compounds and compositions for inhibition of FASN 发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:US-12336981-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; DRAGOVICH Peter; GOSSELIN FRANCIS; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; ROTH BRUCE; SMITH CHASE C; WANG ZHONGGUO; YUEN PO-WAI; ZHENG XIAOZHANG 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:US-11091490-B2 优先权日:2016-11-30 标 题:3-amino-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-ones as cyclin dependent kinase inhibitors 发明人:WUNDERLECH WINFRIED; HUBER LUKAS A; LEBAN JOHANN JAKOB; PATÓ JÃ?NOS; ÖRFI LÃ?SZLÓ; FRIGYES WÃ?CZEK; BÃ?NHEGYI PÉTER; SÃ?POS ANNA; SZÃ?NTAI-KIS CSABA 权利人:ONCOTYROL CENTER FOR PERSONALIZED CANCER MEDICINE GMBH; VICHEM CHEMIE KUTATO KORLATOLT FELELOESSEGUE TARSASAG; MEDIZINISCHE UNIV INNSBRUCK 摘要:The present invention relates to 3-amino-pyrazolo[3,4-d]pyrimidin-4-ones, such as for example, N-{4-[1-(2,6-dichloro-4-sulfamoyl-phenyl)-3-dimethylamino-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-ylmethyl]-phenyl}-2-diethylamino-acetamide, particularly useful as cyclin dependent kinase (CDK) inhibitors, pharmaceutical compositions comprising the same and the use thereof in particular in the prophylaxis and/or treatment of cancer and other proliferative diseases. Furthermore, the present invention relates to processes for the synthesis of said 3-aminopyrazolo[3,4d]pyrimidin-4-ones and intermediates to be used in the processes of the present invention.
专利号:US-9676721-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
专利号:US-7615634-B2 优先权日:2003-02-10 标题:4-aminopyrimidine-5-one derivatives 发明人:BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL 权利人:HOFFMANN LA ROCHE 摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
专利号:US-9555039-B2 优先权日:2011-05-09 标题:Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT) 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)
参考文献:10.1007/978-3-642-41504-3_244 摘要:Hirota E, Kuchitsu K, Steimle T, Vogt J, Vogt N. 113 C7H6F2O 1,2-Difluoro-4-methoxybenzene. 2014. In: Molecules Containing Three or Four Carbon Atoms and Molecules Containing Five or More Carbon Atoms. : Springer Berlin Heidelberg; 2014.