专利号:WO-2023233371-A1 优先权日:2022-06-03 标 题:A continuous flow process for synthesis of organic azides 发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE 摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.
专利号:WO-2021260722-A1 优先权日:2020-06-21 标 题:Design, synthesis of novel oxyindole inhibitors of denv rna dependent rna polymerase 发明人:GUNDLA RAMBABU; ASTHANA SHAILENDRA; BHATTACHARYYA SANKAR; MADDIPATI VENKATANARAYANA CHOWDARY; MITTAL LOVIKA; KAUR JASKARAN; RAWAT YOGITA 权利人:TRANSLATIONAL HEALTH SCIENCE AND TECH INSTITUTE; GANDHI INSTITUTE OF TECH AND MANAGEMENT 摘要:The present invention is drawn to novel compounds of formula I, II and III, including any conformational isomeric form, salts and solvates for inhibition of DENV RNA dependent and RNA polymerase. The present invention also discloses a process of synthesis of the compounds, compositions comprising the said compounds and use of the compounds and treatment comprising the compounds of the present invention.
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-5840915-A 优先权日:1990-01-22 标题:Process for the enatioselective synthesis of intermediates used 发明人:LEE THOMAS BING KIN; WONG GEORGE SEUNG-KIT 权利人:HOECHST MARION ROUSSEL INC 摘要:A process for the stereoselective synthesis of [R]- and [S]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-indole-3-acetonitriles comprises reacting racemic and 5-alkoxy-substituted (+/-)-1,3-dimethyloxindoles with a halogenated acetonitrile in the presence of a substituted N-benzyl cinchoninium, quinidinium, cinchonidinium, or quininium catalyst. The resulting alkylated oxindoles can be converted to primary amines by catalytic reduction in the presence of hydrogen gas. One of the primary amines, such as enantiomers of 3-(2-aminoethyl)-1,3-dihydro-1,3-dimethyl-5-methoxy-2H-indol-2-one, can be enriched by contact with a chiral tartaric acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The product can be used in the synthesis of stereospecific forms of physostigmine and related compounds having pharmaceutical activity.
专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:WO-2023102600-A1 优先权日:2021-12-06 标题:Synthesis of amphiphilic block copolymers and polymeric nanofibers produced therefrom 发明人:ZETTERLUND PER B; ISHIZUKA FUMI; KIM HYUN JIN; CHATANI SHUNSUKE; NIINO HIROSHI 权利人:NEWSOUTH INNOVATIONS PTY LTD 摘要:The present disclosure relates to the field of synthesis of block copolymers, and polymeric nanofibers having a core-shell morphology produced therefrom. The present disclosure relates to the field of synthesis of block copolymers where one block is more hydrophobic than the other block and is a different composition. The disclosure also relates to uses of these polymeric nanofibers in various applications, such as reinforcing a polymeric matrix and for coatings applications.
[参考文献]: Kaur M, Et Al. Oxindole: A Chemical Prism Carrying Plethora Of Therapeutic Benefits. Eur J Med Chem. 2016 Nov 10;123:858-894. [参考文献]: Leoni A, Et Al. 2-Indolinone A Versatile Scaffold For Treatment Of Cancer: A Patent Review (2008-2014). Expert Opin Ther Pat. 2016;26(2):149-73. [参考文献]: Ayman M Saleh, Et Al. Synthesis And Biological Evaluation Of New Pyridone-Annelated Isoindigos As Anti-Proliferative Agents. Molecules. 2014 Aug 25;19(9):13076-92. [参考文献]: F Moroni, Et Al. Oxindole In Pathogenesis Of Hepatic Encephalopathy. Lancet. 1998 Jun 20;351(9119):1861. [参考文献]: Gu-Cai Li, Et Al. Synthesis And Receptor Binding Assay Of Indolin-2-One Derivatives As Dopamine D4 Receptor Ligands. Pharmazie. 2015 Aug;70(8):511-4.
合成参考文献
参考文献:10.1007/s00216-010-3471-8 摘要:Roeser J, Bischoff R, Bruins AP, Permentier HP. Oxidative protein labeling in mass-spectrometry-based proteomics. Analytical and Bioanalytical Chemistry. 2010 Feb 13;397(8):3441–55. doi: 10.1007/s00216-010-3471-8. 参考文献:10.1007/s10895-011-0913-4 摘要:Mandal P, Mandal DK. Localization and environment of tryptophans in different structural states of concanavalin A. J Fluoresc. 2011 Nov;21(6):2123–32. doi: 10.1007/s10895-011-0913-4. 参考文献:10.1107/s1600536811007124 摘要:Selvanayagam S, Ravikumar K, Saravanan P, Raghunathan R. 1',1''-Dimethyl-4'-(naphthalen-1-yl)-1,2,3,4-tetra-hydro-naphthalene-2-spiro-3'-pyrrolidine-2'-spiro-3''-indoline-1,2''-dione. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o751. 参考文献:10.1107/s1600536811015418 摘要:Miao Y, Zhang X, Liu C, You J. Tris(3-hy-droxy-imino-1-methyl-indolin-2-one) monohydrate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1291. 参考文献:10.1016/j.tiv.2005.06.047 摘要:Ye C, Sweeny D, Sukbuntherng J, Zhang Q, Tan W, Wong S, Madan A, Ogilvie B, Parkinson A, Antonian L. Distribution, metabolism, and excretion of the anti-angiogenic compound SU5416. Toxicol In Vitro. 2006 Mar;20(2):154–62. doi: 10.1016/j.tiv.2005.06.047.