专利号:US-11427530-B2 优先权日:2018-02-09 标 题 :Synthesis of 4-chlorokynurenines and intermediates 发明人:LEVIN DANIEL; LEEMING PETER; EISENREICH EMERICH; LIU XUEJUN KARL 权利人:VISTAGEN THERAPEUTICS INC 摘要:The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.
专利号:US-7713446-B2 优先权日:2004-06-28 标 题:Synthesis of nanofibers of polyaniline and substituted derivatives 发明人:EPSTEIN ARTHUR J; CHIOU NAN-RONG 权利人:OHIO STATE UNIVERISTY 摘要:Novel, simple methods are presented directed to the synthesis of nanofibers of polyaniline and substituted derivatives. The production of these fibers is achieved via various methods by controlling the concentration of aniline monomer or substituted aniline derivatives or an oxidant in the reaction medium and maintaining said concentration at a level much lower than conventional polyaniline synthesis methods. Methods are disclosed relating to the use of a permeable membrane to control the release of a monomer and/or oxidant as well as a bulk polymerization method.
专利号:EP-1590332-B1 优先权日:2003-01-09 标题:A process for the synthesis of bisbenzimidazoles and their derivatives. 发明人:JAIN AKASH; TAWAR URMILA; CHANDRA RAMESH; DWARAKANATH B S; CHAUDHURY N K; TANDON VIBHA 权利人:UNIV DELHI 摘要:A process for the synthesis of bisbenzimidazoles and its derivations comprising; (i) reacting 5 chloroaniline with zinc dust and acetic anhydride to produce 5 chloroacetanilide; (ii) reacting 5 chloroacetanilide with HN03 to produce 2-nitro-5-chloroacetanilide; (ix) adding sodium methoxide to 2-nitro-5-ch1oroaniline; (x) heating 2-nitro-5-chloroaniline, methyl piperazine, anhydrous K2CO3 and Dimethyl formamide at 100-120°C produce a mixture which is cooled by pouring ice and is filtered to obtain 5-(4'-methylpiperazin-1'-yl)-2-nitroaniline; (xi) treating 5-(4'-methylpiperazin-l'yl)-2-nitroaniline with Pd/C to produce 2-amino-4-(4'-methylpiperazin-1'-yl) aniline; (xii) refluxing a mixture of 2-amino-4-(4'-methylpiperazin-1'yl) aniline and ethyl-4-amino-3-nitrobenzenecarboximidate hydrochloride in presence of ethanol/glacial acetic acid to produce 4-[5'-(4'-methylpiperazin-1'-yl) 15 benzimidazol-2'-yl)-2-nitroaniline; (xiii) treating a solution of 4-[5'-(4'-methylpiperazin-1'-yi) benzimidazol-2'-yl)-2-nitroaniline with palladium on carbon to yield 2-amino-4-[5'-(4'-Methylpiperazin-1'-yl)benzimidazol-2'-yl]aniline; (xiv) heating 2-amino-4-[5'-(4'-Methylpiperazin-1'-yl)benzimidazol-2'-yl]aniline and 3-4-dimethoxy benzaldehyde using nitrobenzene as a solvent at 110-150°C to produce (DMA) i.e 5-(4-methylpiperazin-1-yl)-2-[2'-(3,4-dimethoxyphenyl)-5'-benzimidazolyl] benzimidazole; (ix) heating 2-amino-4-[5'-(4'-Methylpiperazin-1'-yl) benzimidazol-2'-YI] aniline and 5-Formyl-[3-methoxy-4-hydroxy benzimidazole] using nitrobenzene at 110°C to 150°C in presence of argon to produce (TBZ) i.e 5-(4-methylpiperazine-1-yl)-2-[2' (2'-(4-hydroxy-3methoxyphenyl)5'benzimidazolyl) -5'- benzimidazolyl] benzimidazole.
专利号:US-11459427-B1 优先权日:2021-10-07 标题 :Synthesis of polyaniline or derivatives thereof 发明人:ALAMRY KHALID A; KHAN AJAHAR; ASIRI ABDULLAH MOHAMED 权利人:UNIV KING ABDULAZIZ 摘要:Provided are synthesis methods of polymerizing aniline or derivatives thereof. The production of polyaniline or polyaniline derivatives is controlled by the type of oxidant added in the reaction medium. The methods include the step of using a safe and environmentally friendly carbomethyl cellulose (CMC) or modified CMC as an oxidant in the polymerization reaction to produce polyaniline or aniline derivatives. Synthesis methods of producing O-CMC and O-CMC-S oxidants are also provided herein.
专利号:WO-2022123336-A1 优先权日:2020-12-07 标 题 :Chromeno [4,3-b] quinoline compounds and their synthesis by using silicotungstic acid [h4siw12o40] 发明人:HEGDE SUBRAMANYA GOPAL; LOKESH KOODLUR SANNEGOWDA; SHUBHA JAYACHAMARAJAPURA PRANESH; SUSHMA NURANI VISWANATHAN; BASAVARAJU GIRISH; DANAGOUDAR ANANDA; BODA VIJAY KUMAR 权利人:HEGDE SUBRAMANYA GOPAL; LOKESH KOODLUR SANNEGOWDA 摘要:The present invention relates to the development of novel compounds of chromeno [4,3-b] quinolone derivatives. It particularly relates to the development of novel compounds of thiochromeno [4,3-b] quinolone derivatives for the treatment of coronary artery diseases, dyslipidemia, and metabolic syndrome. The present invention also relates to the first synthesis of Silicotungstic -catalyzed Aza-Diels-Alder-reactions (ADAR) with s-prenyl derivatives of α-tetralone, 4-chromanone and Thiochroman-4-one and various substituted amines to deliver cycloadducts in good yield and excellent diastereoselectivity under mild reaction conditions. The invention further relates to the method for the treatment of coronary artery diseases, dyslipidemia, and metabolic syndrome by using synthesized compounds of thiochromeno [4,3-b] quinolone derivatives. The present invention provides the use of Silicotungstic acid as Lewis acid for Aza-Diels-Alder-reactions to get a mixture of diastereomers are the first examples. In addition to its efficiency, simplicity, and mild reaction conditions, the catalyst is very cheap and only a small amount (10 mol%) is needed. Intramolecular cyclization was carried out very conveniently as a one-pot reaction starting from the S-prenyl chromene-3-carbaldehyde and arylamines without isolation of the intermediate imines.
专利号:US-2006052577-A1 优先权日:2001-02-06 标题:Methods of synthesis of polymers and copolymers from natural products 发明人:SWIFT GRAHAM; WESTMORELAND DAVID G; HUGHES KATHLEEN 权利人:SWIFT GRAHAM; WESTMORELAND DAVID G; HUGHES KATHLEEN 摘要:Described are polymers and copolymers containing sorbitol, citric acid, starch, aspartic acid, succinic anhydride, adipic acid mixtures thereof, methods of their synthesis and their uses.
参考标题:Racemization Free Longer N-Terminal Peptide Hydroxamate Synthesis On Solid Support Using Ethyl 2-(Tert-Butoxycarbonyloxyimino)-2-Cyanoacetate 作者:Srinivasa Rao Manne,Kishore Thalluri,Rajat Subhra Giri,Ashim Paul,Bhubaneswar Mandal |发布日期:2015.10 摘要:Protocol For The Synthesis Of Peptide Hydroxamic Acids Directly From Carboxylic/amino Acids By Ethyl 2-(Tert-Butoxycarbonyloxyimino)-2-Cyanoacetate In The Presence Of Dipea/dmap At Room Temperature Is Described. The Compatibility Of This Method With Fmoc Based Solid Phase Peptide Synthesis (Spps) Is Also Demonstrated By Synthesizing Three Relatively Large N-Terminal Peptide Hydroxamic Acids On Resin. Also
合成参考文献
参考文献:10.1107/s1600536811011366 摘要:Shakuntala K, Foro S, Gowda BT. 4-Chloro-N-(3-chloro-phen-yl)benzene-sulfonamide. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1017. 参考文献:10.1107/s1600536811010440 摘要:Saraswathi BS, Foro S, Gowda BT. N,N′-Bis(3-chlorophenyl)succinamide. Acta Crystallogr E Struct Rep Online. 2011 Mar 26;67(4):o966. doi: 10.1107/s1600536811010440. 参考文献:10.1107/s1600536811014425 摘要:Tang JM, Feng ZQ, Cheng W. Bis(4-amino-2-chloro-phen-yl) disulfide. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1197. 参考文献:10.1107/s1600536811014942 摘要:Saraswathi BS, Foro S, Gowda BT. N-(3-Chlorophenyl)-N′-(2-methylphenyl)succinamide monohydrate. Acta Crystallogr E Struct Rep Online. 2011 Apr 29;67(5):o1223. doi: 10.1107/s1600536811014942. 参考文献:10.1107/s1600536811017909 摘要:Bustos C, Alvarez-Thon L, Cárcamo JG, Ibañez A, Sánchez C. 2-[2-(3-Chloro-phen-yl)hydrazinyl-idene]-1,3-diphenyl-propane-1,3-dione. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1450–1.