专利号:US-8138346-B2 优先权日:2006-08-16 标题 :Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG 权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC 摘要:The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. n nThe substituents R, R 5 , R 6 , R 7 , R 8 and R 9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
专利号:US-2013165350-A1 优先权日:2011-12-22 标 题:Surface linkers for array synthesis 发明人:KUIMELIS ROBERT; MCGALL GLENN; PAO DEXTER; CHEN ZIHUI; AXELROD TREVOR 权利人:KUIMELIS ROBERT; MCGALL GLENN; PAO DEXTER; CHEN ZIHUI; AXELROD TREVOR; AFFYMETRIX INC 摘要:The present invention provide several methods of derivatizing a surface of a support with one or more linkers thus providing a suitable platform for synthesis of a polymer array, particular a nucleic acid array. Some methods derivatize a surface with a self-assembled monolayer (SAM) of a linker. The SAM confers advantages of hydrolytic stability, broad compatibility with synthesis and detection chemistries, and reduced emergence of latent functional groups during polymer array synthesis. Substrates can also be derivatized with multi-layers of SAMs providing greater hydrolytic stability. Substrates can also be derivatized by synthesizing a linker in situ on the substrate by atom transfer radical polymerization of functional and functional monomers. Appropriate selection of monomers reduces emergence of latent functional groups in subsequent array synthesis.
专利号:US-2022098155-A1 优先权日:2018-11-14 标 题 :Novel pathway for the synthesis of diazirines, that may or may not be enriched in nitrogen-15 发明人:REBOUL VINCENT; FRANCK XAVIER; GLACHET THOMAS; MARZAG HAMID 权利人:UNIV ROUEN NORMANDIE; UNIV CAEN; INSTITUT NAT DES SCIENCES APPLIQUEES DE ROUEN INSA; CENTRE NAT RECH SCIENT; ECOLE NAT SUPERIEURE DINGENIEURS DE CAEN 摘要:The present invention concerns a novel method for synthesising diazirines, that may or may not be enriched in nitro-gen-15, from amino acids or imines, via a one-pot synthesis method, comprising the reaction of the starting amino acid or imine with ammonia, which may or may not be enriched in nitrogen-15, and a hypervalent iodine oxidant. The present invention also relates to a method for synthesising ammonia enriched in nitrogen-15. The invention also concerns certain diazirines of formula (I) likely to be obtained by the claimed synthesis method, and also refers to the 15 N 2 -diazirines of formula (I′). The claimed diazirines can be used in photoaffinity labelling. The 15 N 2 -diazirines can also be used in hyperpolarisation, in particular in the medical imaging field.
专利号:WO-2021161084-A1 优先权日:2020-02-16 标题 :N-(4-fluorophenyl)-5-phenyl-[1,2,4] triazolo [1,5-a] pyridine-2-carboxamide derivatives and their synthesis thereof 发明人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP 权利人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP 摘要:The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.
专利号:US-2003232996-A1 优先权日:2001-04-20 标题:Regioselective synthesis of 3,4-di{(carboclyl or heterocyclyl)thiophenes 发明人:BROWN DAVID L; LUDWIG CINDY L 摘要:A novel process for preparing 3,4-di(carbocyclyl or heterocyclyl)thiophenes comprising reacting a compound of Formula IV with a ring cyclizing reagent to form the compound of Formula V to yield a compound of Formula V wherein R 1 , R 2 and R 3 are as defined in the specification.
专利号:US-8367819-B2 优先权日:2004-06-10 标 题:Synthesis of caprolactam from lysine 发明人:FROST JOHN W 权利人:UNIV MICHIGAN STATE; FROST JOHN W 摘要:In various embodiments, the present invention can involve a method of synthesizing α-amino-ε-caprolactam. The method can comprise heating a salt of L-lysine in a solvent comprising an alcohol. In other embodiments, the present invention can involve methods for synthesizing ε-caprolactam. The methods can comprise heating a salt of L-lysine in a solvent comprising an alcohol and deaminating the reaction product. In various embodiments, the invention can include methods of converting biomass into nylon 6. The methods can comprise heating L-lysine in a solvent comprising an alcohol to produce α-amino-εcaprolactam, deaminating to produce ε-caprolactam and polymerizing into nylon 6, wherein the L-lysine is derived from the biomass. In other embodiments, the present invention can include methods of making nylon 6. The methods can comprise synthesizing ε-caprolactam and then polymerizing, wherein the ε-caprolactam is derived from L-lysine.
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