专利号:US-2009221834-A1 优先权日:2006-04-20 标题 :Synthesis of 5-Beta-Keto-1,2,4-Oxadiazoles and Conversion of 5-Beta-Keto-1,2,4 Oxadiazoles to N-Pyrazolyl Amidoximes 发明人:JENSEN DAVID R; SIDENSTICK JOHN E 权利人:JENSEN DAVID R; SIDENSTICK JOHN E 摘要:The disclosed invention relates to a process for preparing 5-β-keto-1,2,4-oxadiazoles of formula (I), and conversion of 5-β-keto-1,2,4-oxadiazoles (I) into N-pyrazolyl amidoximes of the formula (II) through reaction with hydrazine. The process is defined by two steps. An amidoxime, which may be prepared in situ, is condensed with a β-keto ester to form a 5-β-keto-1,2,4-oxadiazole. The 5-β-keto-1,2,4-oxadiazole is subsequently reacted with hydrazine to furnish the desired N-pyrazolyl amidoxime. The disclosed invention provides several advantages over the current state of the art for the synthesis of N-pyrazolyl amidoximes, which require the condensation of a pyrzolylamine with an actived substrate and subsequent reaction with hydroxyl amine. N-pyrazolyl amidoximes are useful synthetic intermediates, especially for the preparation of photographic developing chemicals.
专利号:US-7074921-B2 优先权日:2001-11-13 标题 :Process for the preparation of 3,7-disubstituted-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine compounds 发明人:KRONENTHAL DAVID R; BHANDARU RAO S; SHI ZHONGPING; MUDRYK BOGUSLAW M 权利人:BRISTOL MYERS SQUIBB CO 摘要:Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity.
专利号:US-5254558-A 优先权日:1991-08-15 标 题:Substituted 1,3-diazines as leukocyte elastase inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ICI PLC 摘要:The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
专利号:CN-113861119-A 优先权日:2021-11-23 标题:A kind of method for cobalt-catalyzed synthesis of quinoline and quinazoline compounds
专利号:US-7569606-B2 优先权日:2006-01-26 标 题 :Platinum complexes with mononitrile-containing ligands 发明人:XIAO ZEJUN; HAUSHEER FREDERICK H; PETLURU PAVANKUMAR 权利人:BIONUMERIK PHARMACEUTICALS INC 摘要:Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L 1 and L 2 )which can be hydrolyzed iii vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.
专利号:EP-2013190-A2 优先权日:2006-04-20 标题 :SYNTHESIS OF 5-ß-KETO-1,2,4-OXADIAZOLES AND CONVERSION OF 5-ß-KETO-1,2,4-OXADIAZOLES TO N-PYRAZOLYL AMIDOXIMES
[参考文献]: A P Kumar, Et Al. Vibrational Analysis Of Substituted Benzonitriles. Iii. Transferability Of Force Constants--The Case Of Some Halogeno-, Methoxy- And Nitro-Benzonitriles. Spectrochim Acta A Mol Biomol Spectrosc. 1997 Oct 15;53A(12):2041-8. [参考文献]: Andrej Maroz, Et Al. Release Of Nitrite From The Antitubercular Nitroimidazole Drug Pa-824 And Analogues Upon One-Electron Reduction In Protic, Non-Aqueous Solvent. Org Biomol Chem. 2010 Jan 21;8(2):413-8. [参考文献]: B Markus, Et Al. In Vitro Metabolism Of Aromatic Nitriles. J Pharm Sci. 1994 Dec;83(12):1729-34. [参考文献]: G Monechi, Et Al. [参考文献]: Med Lav. 1991 Mar-Apr;82(2):137-41.
合成参考文献
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