专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-10954178-B1 优先权日:2020-08-28 标题 :Synthesis of haloindenes 发明人:WNUK STANISLAW F; HOWLADER MD ABU HASAN 权利人:WNUK STANISLAW F; HOWLADER MD ABU HASAN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides an expedited synthesis of 5, 6, and 7-iodoindenes from the corresponding aminoindan-1-ones in more than 70% yield, employing readily available precursors and reagents. A three-step sequence involves diazotization-iodination of aminoindan-1-one followed by reduction and dehydration. The method has a general character and can be extended for the preparation of various 4-, 5-, 6- or 7-haloindenes using different halogen sources for diazotization-halogenation reaction.
专利号:WO-0142264-A1 优先权日:1999-12-10 标 题 :Method for the synthesis of sialylated oligosaccharide donors 发明人:MEHTA SEEMA; GILBERT MICHEL; WAKARCHUK WARREN W; WHITFIELD DENNIS M 权利人:CA NAT RESEARCH COUNCIL; MEHTA SEEMA; GILBERT MICHEL; WAKARCHUK WARREN W; WHITFIELD DENNIS M 摘要:A method for the synthesis of aryl thioglycosides comprising a sialylated residue of β-D-galactose is disclosed. The method consists of preparing by a chemical synthesis a non-sialylated aryl thioglycoside, and enzymatically sialylating the latter with a sialic acid in the presence of a suitable sialyltransferase. The sialylated aryl thioglycoside is then chemically derivatized by standard procedures, to provide a derivative suitable for use as a donor in chemical syntheses of sialylated oligosaccharides. The derivatized sialylated aryl thioglycosides are prepared in high yields, due to reduced number of chemical and purification steps involved in the process. Derivatized aryl thioglycosides useful as building blocks for the synthesis of biologically active sialylated oligosaccharides are also disclosed.
专利号:US-11168050-B2 优先权日:2014-03-27 标 题 :Efficient synthesis of amines and amides from alcohols and aldehydes by using cascade catalysis 发明人:CÓRDOVA ARMANDO; BERGLUND PER; ANDERSON MATTIAS; AFEWERKI SAMSON 权利人:XP CHEMISTRIES AB 摘要:The present invention relates generally to an eco-friendly methodology for the conversion of alcohols and aldehydes to amines and amides using an integrated enzyme cascade system with metal- and organocatalysis. More specifically, the present invention relates to synthesis of capsaicinoids starting from vanillin alcohol and using a combination of an enzyme cascade system and catalysts. Furthermore, the method also relates to synthesis of capsaicinoids derivatives starting from vanillin alcohol derivatives and using a combination of an enzyme cascade system and catalysts.
专利号:US-2012178710-A1 优先权日:2009-07-01 标题 :Synthesis of cyclic diguanosine monophosphate and thiophosphate analogs thereof 发明人:JONES ROGER A; GAFFNEY BARBARA L 权利人:JONES ROGER A; GAFFNEY BARBARA L; UNIV RUTGERS 摘要:The invention provides methods for the synthesis of cyclic dinucleotides and thiophosphate analogs thereof as well as a new family of analogs of cyclic diguanosine monophosphate that includes a series of seven phosphorothioate derivatives that includes diastereomers of mono-, di-, and trithiophosphates.
专利号:WO-2004046173-A1 优先权日:2002-11-19 标题:Scaffolds useful to the synthesis of compounds with biological activity 发明人:GIANNINI GIUSEPPE; SCOLASTICO CARLO; MANZONI LEONARDO 权利人:SIGMA TAU IND FARMACEUTI; GIANNINI GIUSEPPE; SCOLASTICO CARLO; MANZONI LEONARDO 摘要:The present invention relates to cyclic compounds having the azabicycloalkane structure. Said compounds are useful as intermediates for the synthesis of compounds with biological activity.
1: Liu D, Gao M, Yang Y, Qi YU, Wu K, Zhao S. Inhibition of autophagy promotes cell apoptosis induced by the proteasome inhibitor MG-132 in human esophageal squamous cell carcinoma EC9706 cells. Oncol Lett. 2015 May;9(5):2278-2282. Epub 2015 Mar 17. 2: Hosseini SM, Hajian M, Forouzanfar M, Ostadhosseini S, Moulavi F, Ghanaei HR, Gourbai H, Shahverdi AH, Vosough AD, Nasr-Esfahani MH. Chemically assisted somatic cell nuclear transfer without micromanipulator in the goat: effects of demecolcine, cytochalasin-B, and MG-132 on the efficiency of a manual method of oocyte enucleation using a pulled Pasteur pipette. Anim Reprod Sci. 2015 Jul;158:11-8. doi: 10.1016/j.anireprosci.2015.04.002. Epub 2015 Apr 15. doi: 10.1016/j.biopha.2014.07.011. Epub 2014 Jul 18. doi: 10.1007/s11010-014-2134-z. Epub 2014 Jul 4. 5: Wójcik S, Spodnik JH, Spodnik E, Dziewiątkowski J, Moryś J. Nigrostriatal pathway degeneration in rats after intraperitoneal administration of proteasome inhibitor MG-132. Folia Neuropathol. 2014;52(1):41-55. doi: 10.1016/j.neuint.2013.07.008. Epub 2013 Jul 31. doi: 10.1111/febs.12264. Epub 2013 May 7.
合成参考文献
参考文献:10.1186/1476-4598-9-38 摘要:Lynch JT, Rajendran R, Xenaki G, Berrou I, Demonacos C, Krstic-Demonacos M. The role of glucocorticoid receptor phosphorylation in Mcl-1 and NOXA gene expression. Molecular Cancer. 2010 Feb 15;9(1):38. doi: 10.1186/1476-4598-9-38. 参考文献:10.18632/aging.100003 摘要:Vorovich E, Ratovitski EA. Dual regulation of TERT activity through transcription and splicing by DeltaNP63alpha. Aging (Albany NY). 2008 Dec 09;1(1):58–67. 参考文献:10.1042/bj20091077 摘要:Liou GY, Zhang H, Miller EM, Seibold SA, Chen W, Gallo KA. Induced, selective proteolysis of MLK3 negatively regulates MLK3/JNK signalling. Biochem J. 2010 Apr 14;427(3):435–43. doi: 10.1042/bj20091077. 参考文献:10.1007/s00439-011-1058-x 摘要:Williamson SL, Giudici L, Kilstrup-Nielsen C, Gold W, Pelka GJ, Tam PP, Grimm A, Prodi D, Landsberger N, Christodoulou J. A novel transcript of cyclin-dependent kinase-like 5 (CDKL5) has an alternative C-terminus and is the predominant transcript in brain. Hum Genet. 2012 Feb;131(2):187–200. doi: 10.1007/s00439-011-1058-x.