专利号:US-7148356-B2 优先权日:2001-07-13 标题:Process for the catalytic synthesis of biaryls and polymers from aryl compounds 发明人:SMITH III MILTON R; MALECZKA ROBERT E 权利人:UNIV MICHIGAN STATE 摘要:A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO 2 CF 3 ), or nonaflate (OSO 2 C 4 F 9 ). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.
专利号:US-12172982-B2 优先权日:2020-08-12 标 题:Synthesis of quinazoline compounds 发明人:LIM NGIAP-KIE; SHEN JEFF; SIROIS LAUREN ELIZABETH; TIMMERMAN JACOB C; TRACHSEL ETIENNE; WHITE NICHOLAS ANDREW; XU JIE; ZHANG HAIMING; BACHMANN STEPHAN; BIGLER RAPHAEL; CLAGG KYLE BRADLEY PASCUAL; DIPASQUALE ANTONIO GIOVANNI; GOSSELIN FRANCIS; ORCEL UGO JONATHAN; MEIER ROLAND CHRISTOPH 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.
专利号:US-2018051042-A1 优先权日:2016-08-22 标题 :Methods for forming saturated (hetero)cyclic borylated hydrocarbons and related compounds 发明人:SMITH III MILTON R; SHANNON TIMOTHY M; MALECZKA JR ROBERT E; FORNWALD RYAN M 权利人:UNIV MICHIGAN STATE 摘要:The disclosure relates to methods for forming at least partially saturated cyclic and heterocyclic borylated hydrocarbons, as well as related compounds, which can be precursor compounds in the synthesis of any of a variety of pharmaceutical or medicinal compounds with a desired structure and/or stereochemistry for drug synthesis or drug candidate evaluation. The methods generally include reduction of an unsaturated cyclic or heterocyclic borylated hydrocarbon having a boron-containing substituent at an sp 2 -carbon, where such reduction converts the sp 2 -carbon to an sp 3 -carbon at the point of attachment of the boron-containing substituent. The methods can exhibit a selectivity for syn-addition during reduction, which can provide stereospecific products, such as when the unsaturated cyclic or heterocyclic reactant is multiply substituted with boron groups and/or other functional groups.
专利号:US-7329769-B2 优先权日:2001-07-13 标 题:Catalytic boronate ester synthesis from boron reagents and hydrocarbons 发明人:SMITH III MILTON R 权利人:UNIV MICHIGAN STATE 摘要:A process for producing a ring-substituted arene borane which comprises reacting a ring-substituted arene with an HB organic compound in the presence of a catalytically effective amount of an iridium or rhodium complex with three or more substituents, excluding hydrogen, bonded to the iridium or rhodium and a phosphorus organic ligand, which is at least in part bonded to the iridium or rhodium, to form the ring-substituted arene borane. Also provided are catalytic compounds for catalyzing the process comprising an iridium or rhodium complex with three or substituents, excluding hydrogen, bonded to the iridium or rhodium and optionally, a phosphorus organic ligand, which is at least in part bonded to the iridium or rhodium.
专利号:US-2005182261-A1 优先权日:2001-07-13 标 题:Process for the catalytic synthesis of biaryls and polymers from aryl compounds
专利号:WO-2022035790-A1 优先权日:2020-08-12 标题:Synthesis of quinazoline compounds
参考文献:10.1055/s-0036-1588903 摘要:Stokes S, Alanine T, Scott J. Synthesis of Electron-Deficient N1-(Hetero)aryl 3,3,5,5-Tetramethyl Piperazinones. Synlett. 2016 Oct 20;28(03):357–61. doi: 10.1055/s-0036-1588903.