专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
专利号:US-9856275-B2 优先权日:2013-02-12 标 题:Synthesis and use of fluorinated compounds 发明人:MOLANDER GARY ALAN; ARGINTARU OANA ANDREEA 权利人:UNIV PENNSYLVANIA 摘要:The invention is directed to the preparation of fluorinated compounds and their use in organic synthesis. In particular, the invention is directed to methods of reacting compounds of structure with R f —CHâ•?N 2 or (CF 3 ) 2 Câ•?N 2 to form a perfluoroalkylate or -arylated compounds, and products derived from these reactions, where X, Y B , and R f are described herein.
专利号:EP-1486498-A1 优先权日:1998-11-23 标 题 :Process and intermediates for growth hormone secretagogues 发明人:CHIU CHARLES KWOK-FUNG; GRIFFITH DAVID ANDREW 权利人:PFIZER PROD INC 摘要:This invention relates to a process for preparing compounds of the Formulan nwherein R 1 , R 2 and Pt are as defined in the specification, which are intermediatesnin the synthesis of certain growth hormone secretagogue compounds. Thisninvention further relates to processes for preparing the growth hormonensecretagogues. The invention also relates to the compound of Formula I whereinnR 1 is H, R 2 is 2,2,2-trifluoromethyl and Pt is Boc.
专利号:US-2021069337-A1 优先权日:2018-04-27 标题 :Integrin targeting ligands and uses thereof 发明人:LI ZHEN; CARLSON JEFFREY; NICHOLAS ANTHONY; LI XIAOKAI; SHU DONGXU; FOWLER-WATTERS MATTHEW 权利人:ARROWHEAD PHARMACEUTICALS INC 摘要:Compounds having affinity for integrins, the synthesis of these compounds, and the use of these compounds as ligands to facilitate the delivery of cargo molecules to cells expressing integrins are described. The described integrin targeting ligands have serum stability and affinity for αvβ3 integrin and/or αvβ5 integrin, and are suitable for conjugation to cargo molecules, such as such as oligonucleotide-based therapeutic agents (e.g., RNAi agents), to facilitate delivery of the cargo molecules to cells and tissues, such as tumor cells, that express integrin αvβ3, integrin αvβ5, or both integrin αvβ3 and integrin αvβ5. Compositions that include integrin targeting ligands and methods of use are also described.
专利号:US-6686471-B2 优先权日:1998-11-23 标 题:Process and intermediates for growth hormone secretagogues 发明人:CHIU CHARLES K; GRIFFITH DAVID A 权利人:PFIZER 摘要:This invention relates to a process for preparing compounds of the Formula I, n wherein R 1 , R 2 and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R 1 is H, R 2 is 2,2,2-trifluoromethyl and Pt is Boc.
专利号:EP-1004583-B1 优先权日:1998-11-23 标题:Process and hydantoin intermediates for the synthesis of growth hormone secretagogues
[参考文献]: Quincy Laron Ford, Et Al. Aqueous In Situ Derivatization Of Carboxylic Acids By An Ionic Carbodiimide And 2,2,2-Trifluoroethylamine For Electron-Capture Detection. J Chromatogr A. 2007 Mar 23;1145(1-2):241-5.
合成参考文献
摘要:S100 | PFASREACH | List of PFAS identified in REACH 2019 | DOI:10.5281/zenodo.7426856 摘要:Fluorine Chemistry, Volume III. Biological Effects of Organic Fluorides, Simons, J.H., ed., New York, Academic Press, Inc., 1963, 3(81), 1963