1H-imidazoletert-butyl (1-chloroethyl) carbonate1,2,2,2-Tetrachloroethyl tert-Butyl Carbonate1,1'-carbonyldiimidazoledipercarbonate de O,O-t-butylepercarbonate de O,O-t-butyle et O-t-butyle1-tert-butyl 3-methyl 2,2-dimethylmalonate1H-imidazole
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-6455680-B1 优先权日:2000-12-21 标 题 :Methods utilizing aryl thioimines in synthesis of erythromycin derivatives 发明人:LUKIN KIRILL A 权利人:ABBOTT LAB 摘要:An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:WO-2025027521-A1 优先权日:2023-08-01 标题 :An improved process for the preparation of avibactam and intermediate thereof 发明人:DHAVARIA SANDEEP; HANDA VISHAL; SHARMA SUNEEL KUMAR; MEHTA ANSHU KUMAR; SINGH ADITYA NARAYAN; ABUL AZIM; GUPTA NITIN; SINGH GOVIND; CABRI WALTER 权利人:FRESENIUS KABI ONCOLOGY LTD 摘要:The present invention relates to an improved process for the preparation of Avibactam or a pharmaceutically acceptable salt thereof, particularly the present invention relates to process for the preparation of a bridged ester intermediate of Formula I, wherein R1 is a hydroxy protecting group which is a key intermediate for Avibactam or a pharmaceutically acceptable salt thereof. The present invention also relates to the crystalline form of intermediates used for the synthesis of Avibactam or a pharmaceutically acceptable salt thereof. The invention also provides improved processes for the preparation of Avibactam or a pharmaceutically acceptable salt, using the bridged ester compound of formula I prepared by the process of the present invention.
专利号:US-7074932-B2 优先权日:1999-06-24 标题 :Preparation of quinoline-substituted carbonate and carbamate derivatives 发明人:ALLEN MICHAEL S; PREMCHANDRAN RAMIYA H; CHANG SOU-JEN; CONDON STEPHEN; DEMATTEI JOHN A; KING STEVEN A; KOLACZKOWSKI LAWRENCE; MANNA SUKUMAR; NICHOLS PAUL J; PATEL HEMANT H; PATEL SUBHASH R; PLATA DANIEL J; STONER ERIC J; TIEN JIEN-HEH J; WITTENBERGER STEVEN J 权利人:ALLEN MICHAEL S; PREMCHANDRAN RAMIYA H; CHANG SOU-JEN; CONDON STEPHEN; DEMATTEI JOHN A; KING STEVEN A; KOLACZKOWSKI LAWRENCE; MANNA SUKUMAR; NICHOLS PAUL J; PATEL HEMANT H; PATEL SUBHASH R; PLATA DANIEL J; STONER ERIC J; TIEN JIEN-HEH J; WITTENBERGER STEVEN J 摘要:The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.
专利号:US-2018051042-A1 优先权日:2016-08-22 标题 :Methods for forming saturated (hetero)cyclic borylated hydrocarbons and related compounds 发明人:SMITH III MILTON R; SHANNON TIMOTHY M; MALECZKA JR ROBERT E; FORNWALD RYAN M 权利人:UNIV MICHIGAN STATE 摘要:The disclosure relates to methods for forming at least partially saturated cyclic and heterocyclic borylated hydrocarbons, as well as related compounds, which can be precursor compounds in the synthesis of any of a variety of pharmaceutical or medicinal compounds with a desired structure and/or stereochemistry for drug synthesis or drug candidate evaluation. The methods generally include reduction of an unsaturated cyclic or heterocyclic borylated hydrocarbon having a boron-containing substituent at an sp 2 -carbon, where such reduction converts the sp 2 -carbon to an sp 3 -carbon at the point of attachment of the boron-containing substituent. The methods can exhibit a selectivity for syn-addition during reduction, which can provide stereospecific products, such as when the unsaturated cyclic or heterocyclic reactant is multiply substituted with boron groups and/or other functional groups.
参考标题:Alkyl 1-Chloroalkyl Carbonates: Reagents For The Synthesis Of Carbamates And Protection Of Amino Groups 作者:Gérard Barcelo,Jean-Pierre Senet,Gérard Sennyey,Jean Bensoam,Albert Loffet 摘要:The Synthesis Of 1-Chloroalkyl Carbonates And Their Reaction With Various Type Of Amines Are Described. This Reaction Is Useful For The Synthesis Of Carbamate Pesticides And For The Protection Of Various Amino Groups, Including Amino Acids.
合成参考文献
参考文献:10.1055/s-2006-939689 摘要:Rama Rao K, Somi Reddy M, Narender M, Nageswar Y. N-Boc Protection of Amines with Di-tert-butyldicarbonate in Water under Neutral Conditions in the Presence of β-Cyclodextrin. Synlett. 2006 Apr 24;2006(07):1110–2. doi: 10.1055/s-2006-939689.