专利号:US-7507843-B2 优先权日:2003-10-16 标题:Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:SONG JINHUA J; TAN ZHULIN; XU JINGHUA; YEE NATHAN K; SENANAYAKE CHRIS H 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:A process for stereoselective synthesis of compounds of Formula X wherein: R1 is an aryl or heteroaryl group, each optionally independently substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, C3-C8 cycloalkyl, heterocyclyl, aryl, heteroaryl, C1-C5 alkoxy, C2-C5 alkenyloxy, C2-C5 alkynyloxy, aryloxy, C1-C5 alkanoyloxy, C1-C5 alkanoyl, aroyl, trifluoromethyl, trifluoromethoxy, or C1-C5 alkylthio, wherein each substituent group of R1 is optionally independently substituted with one to three substituent groups selected from methyl, methoxy, fluoro, chloro, hydroxy, oxo, cyano, or amino; and R2 and R3 are each independently hydrogen or C1-C5 alkyl, or R2 and R3 together with the carbon atom they are commonly attached to form a C3-C8 spiro cycloalkyl ring.
专利号:US-2004014168-A1 优先权日:1998-06-11 标题:Reagents and methods for library synthesis and screening 发明人:SCHREIBER STUART L; BLACKWELL HELEN E; PEREZ FERNANDEZ LUCY; TALLARICO JOHN A 权利人:HUGHES HOWARD MED INST 摘要:The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 μm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. n The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
专利号:US-8716507-B2 优先权日:2008-10-31 标题 :Iron(II) catalysts containing diimino-diphosphine tetradentate ligands and their synthesis 发明人:MIKHAILINE ALEXANDRE; FREUTEL FRIEDERIKE; SUI-SENG CHRISTINE; MEYER NILS; MORRIS ROBERT H; LAGADITIS PARASKEVI OLYMPIA 权利人:MIKHAILINE ALEXANDRE; FREUTEL FRIEDERIKE; SUI-SENG CHRISTINE; MEYER NILS; MORRIS ROBERT H; LAGADITIS PARASKEVI OLYMPIA; GOVERNING COUNCIL OF UNIVERSITY OF TORONTO 摘要:New hexa-coordinate iron (II) complexes comprising compounds of formula (I) are described. These compounds comprise a tetradentate ligand with donor atoms comprising nitrogen and phosphorus. These complexes are shown for the first time to be useful catalysts for the hydrogenation of ketones, aldehydes, or imines to produce alcohols or amines, and the asymmetric hydrogenation of prochiral ketones or imines to produce non-racemic alcohols or amines. The source of the hydrogen can be hydrogen gas or a hydrogen-donating molecule such as isopropanol or hydrogen-donating mixture such as formic acid and an amine depending on the structure of the catalyst. In certain embodiments, the axial ligands on the catalyst comprise organonitrile ligands, carbonyl ligands, isonitrile ligands, or combinations thereof. The catalysts and the preparation thereof are disclosed. A reaction using phosphine and diamine precursors that is templated by the iron ion is the preferred route to the catalysts.
专利号:US-5231198-A 优先权日:1992-07-06 标题:Asymmetric synthesis of hexahydrodibenzofurans by stereospecific inversion of ortho substituted 2-phenylcyclohexanols 发明人:POWERS MATTEW R; GOLEC FREDERICK A 权利人:RHONE POULENC RORER PHARMA 摘要:This invention relates to the stereospecific process for the preparation, separation and purification of hexahydrodibenzofurans which are used in the preparation of the 5HT 3 compounds. More specifically, the present invention relates to a process for the preparation of substantially optically pure cishexahydrodibenzofuran compounds including at least two chiral fused ring centers which comprises the acidic catalyzed stereospecific ring closure by the intra-molecular inversion of a gamma, i.e. 2', carbon atom of a 2-[(2'-leaving group)cycloalkyl]phenol.
专利号:US-4847429-A 优先权日:1987-08-03 标 题:Synthesis of phenylhydroquinones 发明人:LENTZ CARL M; GUSTAFSON BRUCE L; VAN SICKLE DALE E; BOWERS JR JOSEPH S 权利人:EASTMAN KODAK CO 摘要:Process is disclosed for the preparation of phenylhydroquinones by the alkylation of hydroquinone (or derivatives thereof) with the cyclohexyl moieties, cyclohexanol or cyclohexene (or derivatives thereof), followed by dehydrogenation of the intermediate cyclohexylhydroquinone.
专利号:US-6147159-A 优先权日:1998-09-30 标 题 :Compositions for organic synthesis on solid phase and methods of using the same 发明人:HU YONGHAN; LABADIE JEFFREY W; PORCO JR JOHN ANTHONY; TROST BARRY MARTIN 权利人:ARGONAUT TECHNOLOGIES 摘要:A modified solid support for use in solid phase synthesis which comprises: a solid support having a linker group extending therefrom having the general formula: wherein R1 and R2 are each independently selected from the group consisting of alkyl, cycloalkyl, aryl, alkoxy, aryloxy, fluorine, chlorine, iodine and bromine.