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-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-4334079-A 优先权日:1980-11-03 标 题:Synthesis of substituted benzyl esters 发明人:GREENE JAMES M; BUNNELL CHARLES A 权利人:LILLY CO ELI 摘要:A process for preparing certain substituted benzyl esters of phenylacetic acids by esterification in a solvent in which the salt of the acid is insoluble, and in the presence of a phase transfer catalyst.
专利号:WO-2023137518-A1 优先权日:2022-01-21 标题 :Platinum complexes 发明人:ALDRICH-WRIGHT JANICE; GORDON CHRISTOPHER; DEO KRISHANT M; KHOURY ALEEN; MCGHIE BRONDWYN; APUTEN ANGELICO; PLATTEN-MENTI MARIA; RASHID FATIN; JURISINEC ASHLEY; SOLIMAN SARAH 权利人:WESTERN SYDNEY UNIV 摘要:The present disclosure relates to platinum complexes, and in particular platinum(II) and platinum(IV) complexes. The present disclosure also relates to synthesis of the platinum complexes, and to intermediates for the synthesis of the platinum complexes. The present disclosure also relates to methods and use of the platinum complexes for treating cancer.
专利号:US-2013261317-A1 优先权日:2010-09-27 标题 :Methods for preparing synthetic bile acids and compositions comprising the same 发明人:MORIARTY ROBERT M; RAO PHOTON 权利人:MORIARTY ROBERT M; RAO PHOTON; KYTHERA BIOPHARMACEUTICALS INC 摘要:This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C 14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.
专利号:CN-106518822-B 优先权日:2016-10-31 标题 :Synthesis of strigolactone (±)-GR24 and 4-substituted (±)-GR24
[参考文献]: Jonathan M Fitzsimmons, Et Al. Synthesis And σ1 Receptor Binding Of Halogenated N,N'-Diphenethylethylenediamines. Med Chem (Los Angeles). 2011 Dec 25;1(102):1000102.
合成参考文献
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