专利号:US-2015336866-A1 优先权日:2013-01-01 标题:Synthesis of difluoromethyl ethers and sulfides 发明人:HARTWIG JOHN; FIER PATRICK 权利人:UNIV CALIFORNIA 摘要:The synthesis of difluoromethyl ethers and sulfides with a simple, non-ozone-depleting reagent is described. The difluoromethylation of phenols with this reagent occurs at room temperature within minutes with exceptional functional group tolerance. The mild conditions makes possible tandem processes for the conversion of aryl boronic acids, aryl halides and arenes to difluoromethyl ethers. Mechanistic studies support a reaction pathway involving nucleophilic attack of the phenolate to difluorocarbene.
专利号:US-10927135-B2 优先权日:2017-08-03 标 题:Metal-free direct arylation of dialkyl phosphonates for the synthesis of mixed alkyl aryl phosphonates 发明人:KANG JUN YONG; HUANG HAI 权利人:THE BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIV OF NEVADA LAS VE 摘要:Provided herein are phosphates, thiophosphates, phosphonates, and phosphinates, methods of making same, and methods of using these compounds and methods for the generation of pharmaceutically relevant phosphate, phosphonate, and phosphinate analogs. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-12319712-B2 优先权日:2018-05-09 标 题:Methods of synthesizing a polynucleotide array using photoactivated agents 发明人:RAJASEKARAN JOHN J; JAYARAMAN VASANTH; VENUGOPAL ANIRUDH; BEI KANG; WANG TIANHAO; KRISHNA KARTHIK; KRISHNAMURTHY HARI KRISHNAN 权利人:VIBRANT HOLDINGS LLC 摘要:Described herein are methods for the synthesis of DNA polynucleotides and polynucleotides, as well as methods for their deprotection and methods for the use of said compounds and compositions comprising said compounds. In particular, such compounds and compositions comprising them are used in methods for light-directed synthesis of DNA microarrays.
专利号:US-2023357286-A1 优先权日:2020-07-24 标 题:Ketone synthesis and applications 发明人:KISHI YOSHITO; UMEHARA ATSUSHI 权利人:HARVARD COLLEGE 摘要:Provided are new nickel./zirconium-mediated coupling reactions useful in the synthesis of ketone-containing compounds, e.g., halichondrin natural products and related molecules. A feature of the present disclosure is the use of a nickel(I) catalyst in tandem with a nickel (II) catalyst in the Ni/Zr-mediated coupling reactions. Without wishing to be bound by any particular theory, the nickel (I) catalyst selectively activates the electrophilic coupling partner (i.e., the compound of Formula (A)), and the nickel(ll) catalyst selectively activates the nucleophilic coupling partner (i.e., a thioester of Formula (B)). This dual catalyst system leads to improved coupling efficiency and eliminates the need for a large excess of one of the coupling partners (i.e., a compound of Formula (A) or (B)).
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-5530125-A 优先权日:1992-02-25 标 题 :Synthesis of α-substituted-aryl ethylamines 发明人:BERGER JOEL G; CHANG WEI K; KOZLOWSKI JOSEPH A; ZHOU GUOWEI 权利人:SCHERING CORPORTION 摘要:PCT No. PCT/US93/01425 Sec. 371 Date Aug. 19, 1994 Sec. 102(e) Date Aug. 19, 1994 PCT Filed Feb. 23, 1993 PCT Pub. No. WO93/16997 PCT Pub. Date Sep. 2, 1993.A novel process for the preparation of alpha -substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the alpha -carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R4-X, wherein R4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The alpha -substituted arylacetamides are useful as intermediates in the preparation (by reduction) of alpha -substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R4 is 1-(1-cycloalkenyl) are novel.
[参考文献]: Xuebin Liao, Et Al. Enantioselective Alpha-Arylation Of Ketones With Aryl Triflates Catalyzed By Difluorphos Complexes Of Palladium And Nickel. J Am Chem Soc. 2008 Jan 9;130(1):195-200.
合成参考文献
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