专利号:US-4446078-A 优先权日:1982-01-21 标 题 :Process for the preparation of α,α-difluoroalkyl-thiophenyl ketones 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of alpha , alpha -difluoroalkoxy or alpha , alpha -difluoroalkylthiophenyl ketones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a carboxylic acid, a precursor or a derivative of this acid in the presence of boron trifluoride in such an amount that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-4552984-A 优先权日:1982-01-21 标题 :Process for preparation of α,α-difluoroalkoxy or α,.alpha. 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of alpha , alpha -difluoroalkoxy or alpha , alpha -difluoroalkylthiophenyl sulfones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a sulfonic acid, a derivative or a precursor of this acid, in the presence of boron trifluoride in an amount such that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-4438043-A 优先权日:1982-04-22 标题:Process for preparation of di- or trifluoromethoxyphenyl ketones or di- or trifluoromethylthiophenyl ketones 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of di- or trifluoromethoxyphenyl ketones or di- or trifluoromethylthiophenyl ketones, characterized in that, in a first stage, a di- or trihalomethoxybenzene or a di- or trihalomethylthiobenzene is reacted with a trihalomethylated aromatic or aliphatic compound in the presence of boron trifluoride in an amount such that the absolute pressure of boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent and in that, in a second stage, the product of the first stage is hydrolyzed. The resultant products are useful as intermediates in the synthesis of compounds having a pharmaceutical or phytosanitary (e.g., herbicidal) activity.
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-9169209-B2 优先权日:2011-05-04 标题:Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; 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 composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
[参考文献]: F Aladar Bencsath, Et Al. Screening For Petrochemical Contamination In Seafood By Headspace Solid-Phase Microextraction Gas Chromatography-Mass Spectrometry. Anal Bioanal Chem. 2015 May;407(14):4079-90.
合成参考文献
摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 217. 参考文献:10.1038/ncomms14353 摘要:Lin J, Li Z, Kan J, Huang S, Su W, Li Y. Photo-driven redox-neutral decarboxylative carbon-hydrogen trifluoromethylation of (hetero)arenes with trifluoroacetic acid. Nature Communications. 2017 Feb 06;8(1):14353. doi: 10.1038/ncomms14353.