专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:WO-2024036115-A1 优先权日:2022-08-08 标题:Continuous flow synthesis of lorazepam 发明人:THOMPSON DAVID; BIYANI SHRUTI; HYUN SEOK-HEE; MCGUIRE MICHAEL 权利人:PURDUE RESEARCH FOUNDATION; CONTINUITY PHARMA LLC 摘要:A method for synthesis of Lorazepam in a continuous flow using continuous flow reactor, in which method comprises five steps including N-acylation, diazepine ring closure, imine N- oxidation, Polonovski-type rearrangement, and ester hydrolysis; a green reagent comprising a peroxide reagent and rhenium oxide catalyst for N-oxidation of delorazepam; and an ammonium source combination for the synthesis of delorazepam.
专利号:US-4515920-A 优先权日:1984-04-30 标题 :Synthesis of peptides and proteins 发明人:ERICKSON BRUCE W 权利人:UNIV ROCKEFELLER 摘要:Solid phase synthesis of peptides and proteins have been improved by the use of a trifunctional segment, one functional group of which is bound to a solid support, the other two functional groups being available as substrates upon which identical proteins are synthesized.
专利号:US-7098354-B2 优先权日:2002-10-25 标 题:Racemoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indeyl)zirconium compounds 发明人:DAMRAU HANS-ROBERT; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a specific process for the diastereoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indenyl)zirconium compounds of the formula I, n nby reacting the silyl-bridged bisindenyl ligand with a dihalozirconium bis(3,5-di-tert-butylphenoxide)-base adduct to form the diorganosilylbis(2-methylbenzo[e]indenyl)zirconium bis(3,5-di-tert-butylphenoxide) and subsequently replacing the phenoxide groups by X using suitable replacement reagents to give the compound of the formula I; where the substituents X can be identical or different and are each F, Cl, Br, I or linear, cyclic or branched C 1-10 -alkyl; and the substituents R can be identical or different and are each linear, cyclic or branched C 1-10 -alkyl or C 6-10 -aryl; and also to the use of these compounds as catalysts.
专利号:EP-1383732-B1 优先权日:2001-05-04 标题:Labelling reagents, method for synthesis of said reagents and methods for detecting biological molecules 发明人:BOURGET CECILE; LHOMME JEAN; LAAYOUN ALI; KOTERA MITSUHARU; TREVISIOL EMMANUELLE; MENOU LIONEL; BERNAL MENDEZ ELOY 权利人:BIO MERIEUX; UNIV GRENOBLE 1; CENTRE NAT RECH SCIENT 摘要:The invention concerns a temperature-stable labelling reagent of formula (I), wherein: R<1> represents H or an alkyl, aryl or substituted aryl group; R<2> represents a detectable marker or at least two detectable markers linked together by at least a multimeric structure; L is a linking arm comprising a linear catemer concatenation of at least two covalent bonds; and n is an integer equal to 0 or 1; R<3> and R<4> represent, independently of each other: H, NO2, Cl, Br, F, I, R<2>-(L)n-Y-X-, OR, SR, NR2, R, NHCOR, CONHR, COOR with R = alkyl or aryl, A is a linking arm comprising at least a double bond enabling the conjugation of the diazo function with the aromatic cycle; and u is a whole number between 0 and 2, preferably between 0 and 1; and -Y-X- represents -CONH-, -NHCO-, -CH2O-, -CH2S-. The invention also concerns a method for the synthesis of said markers and uses for labelling biological molecules, in particular nucleic acids, with a labelling reagent bearing the diazomethyl function. The invention is particularly applicable in the field of diagnosis.
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 316. 摘要:Zhang, J., Science of Synthesis Knowledge Updates, (2013) 2, 250. 摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2013) 2, 290. 参考文献:10.1021/bc049979u 摘要:Kuhnast B, de Bruin B, Hinnen F, Tavitian B, Dollé F. Design and Synthesis of a New [18F]Fluoropyridine-Based Haloacetamide Reagent for the Labeling of Oligonucleotides: 2-Bromo-N-[3-(2-[18F]fluoropyridin-3-yloxy)propyl]acetamide. Bioconjugate Chem. 2004 May 01;15(3):617–27. doi: 10.1021/bc049979u. 参考文献:10.1107/s010827010302732x 摘要:Blake AJ, Lippolis V, Schröder M. Intramolecular cyclization of 4,7-bis(2-bromoacetyl)-1-thia-4,7-diazacyclononane. Acta Crystallogr C Cryst Struct Commun. 2003 Dec 20;60(1):o100–2. doi: 10.1107/s010827010302732x.