专利号:WO-2016147205-A1 优先权日:2015-03-13 标题 :Novel substituted 3-spirophosphoryl pyrazole-2-oxindoles as anti-infectives and process for the synthesis thereof 发明人:SURYAVANSHI GURUNATH MALLAPPA; SHELKE ANIL MARUTI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to novel substituted 3-spirophosphoryl, pyrazole-2-oxindoles of Formula (I) and its pharmaceutically acceptable salts, esters, ethers, isomers, stereoisomers, positional isomers and pplymorphs. The present invention further relates to one pot, one step process for the synthesis of spirophosphoiyl pyrazole oxindoles of Formula (I) with yield in the range of 70-85%.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-8497296-B2 优先权日:2011-03-31 标 题:N,N′-hydrazino-bis-isatin derivatives with selective activity against multidrug-resistant cancer cells 发明人:HASSAN TAREK ABOUL-FADL MOHAMED; KADI ADNAN AHMED; ABDEL-AZIZ HATEM ABDEL-KHADER 权利人:HASSAN TAREK ABOUL-FADL MOHAMED; KADI ADNAN AHMED; ABDEL-AZIZ HATEM ABDEL-KHADER; UNIV KING SAUD 摘要:The invention is directed to a compound of Formula (I), n nwherein R is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; R 1 is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; X is selected from the group consisting of hydrogen atom or halogen atom; and Y is selected from the group consisting of hydrogen atom, halogen atom, C 1 -C 4 alkyl group, nitro group, and —OCF 3 group, as well as for its use in therapy, preferably for the treatment of cancer, and to a related pharmaceutical composition, the use of the compound for the manufacture of a medicament for the respective medical indication, and a method of synthesis of the compounds of the invention.
专利号:US-8933248-B2 优先权日:2012-06-21 标 题:3-substituted-3-hydroxy oxindole derivatives and process for preparation thereof 发明人:RAO MANDAPATI MOHAN; PRATHIMA PARVATHANENI SAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to expedient method for synthesis of 3-substituted-3-hydroxy-oxindole derivatives, which are useful as synthetic precursors to valuable pharmaceutical compounds. These are synthesized by reacting nitromethane with the corresponding isatins of formula (I). The reaction process of isatins was carried using water as a solvent at room temperature to form the corresponding 3-hydroxy-3-nitromethylindolin-2-ones of formula (II).
专利号:US-7149280-B2 优先权日:2002-12-23 标 题 :Synthesis and screening of ligands using X-ray crystallography 发明人:JHOTI HARREN; CONGREVE MILES STUART; O'REILLY MARC; WYATT PAUL GRAHAM 权利人:ASTEX THERAPEUTICS LTD 摘要:A method for identifying a ligand of a target macromolecule is disclosed, comprising the steps of: soaking one or more crystals of the target macromolecule in a solution containing a collection of compounds generated in situ or separate from the crystal, where the solution has been prepared without the purification of the synthesized collection of compounds; obtaining an X-ray crystal diffraction pattern of the soaked macromolecule crystal; and using said X-ray crystal diffraction pattern to identify any compound bound to the macromolecule crystal, said compound being a ligand of the target macromolecule.
专利号:US-8987195-B2 优先权日:2012-08-08 标 题:HCV NS3 protease inhibitors 发明人:BARA THOMAS; BHAT SATHESH; BISWAS DIPSHIKHA; BROCKUNIER LINDA; BURNETT DUANE A; CHACKALAMANNIL SAMUEL; CHELLIAH MARIAPPAN V; CHEN AUSTIN; CLASBY MARTIN; COLANDREA VINCE J; GUO ZHUYAN; HAN YONGXIN; JAYNE CHARLES; JOSIEN HUBERT; MARCANTONIO KAREN; MIAO SHOUWU; NEELAMKAVIL SANTHOSH; PINTO PATRICK; RAJAGOPALAN MURALI; SHAH UNMESH; VELAZQUEZ FRANCISCO; VENKATRAMAN SRIKANTH; XIA YAN 权利人:MERCK SHARP & DOHME; MERCK CANADA INC 摘要:The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
参考标题:Autoxidation/aldol Tandem Reaction Of 2-Oxindoles With Ketones: A Green Approach For The Synthesis Of 3-Hydroxy-2-Oxindoles 作者:Qing-Bao Zhang,Wen-Liang Jia,Yong-Liang Ban,Yong Zheng,Qiang Liu,Li-Zhu Wu |发布日期:2016.2.18 摘要:In The Presence Of Tetrabutylammonium Fluoride And Molecular Sieves (Ms) 4 å In Dmf, An Efficient Autoxidation Reaction Of 2‐oxindoles With Ketones Under Air At Room Temperature Has Been Developed. This Approach May Provide A Green, Practical, And Metal‐free Protocol For A Wide Range Of Biologically Important 3‐hydroxy‐3‐(2‐oxo‐alkyl)‐2‐oxindoles.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 335. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 344. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 329. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 336. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 346.