专利号:US-2023278959-A1 优先权日:2020-05-04 标题:Synthesis of Optically Active Indoline Derivatives Via Ruthenium(II)-Catalyzed Enantioselective C-H Functionalization 发明人:CUI XIN; LI ZHONG-YUAN; CHAMINDA LAKMAL HETTI HANDI 权利人:UNIV MISSISSIPPI STATE 摘要:Provided herein are a method of Ru(II)-catalyzed enantioselective synthesis of a cyclic compound and cyclic compounds formed therefrom. The method includes providing a precursor compound having an unfunctionalized C—H bond and activating the unfunctionalized C—H bond by reacting the precursor compound in the presence of co-catalysts including a Ru(II) arene complex and a chiral transient directing group (CTDG).
专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
专利号:US-12122759-B2 优先权日:2017-11-07 标 题:Method for the synthesis of cyclic depsipeptides 发明人:HEIMBACH DIRK; OMURA SATOSHI; SUNAZUKA TOSHIAKI; HIROSE TOMOYASU; NOGUCHI YOSHIHIKO; Köbberling Johannes; WU ZHIJIE; FU SHUIBIAO; WU WEI; QIU JINFENG; HE LIU; WEI XUDONG 权利人:ELANCO ANIMAL HEALTH GMBH; THE KITASATO INST 摘要:The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.
专利号:US-2016222024-A1 优先权日:2013-09-20 标 题:S-enantiomer of tetracyclic indole derivative as pbr ligands 发明人:TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER 权利人:GE HEALTHCARE LTD 摘要:The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
专利号:WO-2025058704-A1 优先权日:2023-09-15 标 题:Process for the preparation of epinephrine and norepinephrine 发明人:YUE TAI-YUEN; SAHANI RAJKUMAR; JAYARAMAN ARAVINDAN; DONSBACH KAI; SENANAYAKE CHRIS; QU BO; SIRASANI GOPAL; MANGUNURU HARI; JANGANATI VENUMADHAV; GANGU ARAVIND; TERRAB LEILA; KALIKINIDI NAGESWARA 权利人:UNIV VIRGINIA COMMONWEALTH 摘要:A method of preparing epinephrine or norepinephrine is provided. The method includes reacting a starting material comprising 2-chloro-l-(3,4-dihydroxyphenyl)ethan-l- one with an amine nucleophile RNH2 (R=H for the synthesis of epinephrine or Me for the synthesis of norepinephrine) under conditions suitable for nucleophilic substitution of the starting material to form a substituted starting material and reacting the substituted starting material with a tethered ligand transition metal catalyst under conditions suitable for transfer¬ hydrogenation to produce epinephrine or norepinephrine.
专利号:US-8242277-B2 优先权日:2006-12-12 标题:Preparation of tetrahydroisoquinolines from dihydroisoquinolines 发明人:CANTRELL GARY L; MAGPARANGALAN DAN P; MOSER FRANK W; BAO JIAN; GROTE CHRISTOPHER W; WANG PETER X 权利人:CANTRELL GARY L; MAGPARANGALAN DAN P; MOSER FRANK W; BAO JIAN; GROTE CHRISTOPHER W; WANG PETER X; MALLINCKRODT LLC 摘要:The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
参考标题:Application Of Tethered Ruthenium Catalysts To Asymmetric Hydrogenation Of Ketones, And The Selective Hydrogenation Of Aldehydes 作者:Katherine E. Jolley,Antonio Zanotti‐gerosa,Fred Hancock,Alan Dyke,Damian M. Grainger,Jonathan A. Medlock,Hans G. Nedden,Jacques J. M. Le Paih,Stephen J. Roseblade,Andreas Seger,Vilvanathan Sivakumar,Ivan Prokes,David J. Morris,Martin Wills |发布日期:2012.9.17 摘要:An Improved Method For The Synthesis Of Tethered Ruthenium(II) Complexes Of Monosulfonylated Diamines Is Described, Together With Their Application To The Hydrogenation Of Ketones And Aldehydes. The Complexes Were Applied Directly, In Their Chloride Form, To Asymmetric Ketone Hydrogenation, To Give Products In Excess Of 99% Ee In The Best Cases, Using 30 Bar Of Hydrogen At 60 °C, And To The Selective