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:US-12269790-B1 优先权日:2022-04-29 标题:Process for the preparation of 2,4,6-triiodophenol derivatives 发明人:BARANYAI ZSOLT; GUIDOLIN NICOL; LAZZARI FEDERICA; UGGERI FULVIO 权利人:BRACCO IMAGING SPA 摘要:The invention relates to a process for the preparation of a 2,4,6-triiodo-phenol derivative of formula (II), which is useful as an intermediate for the synthesis of conventional X-ray contrast agents, said process comprising the tri-iodination of the correspondent phenol derivative of said 2,4,6-triiodo-phenol derivative by means of an iodinating system comprising I 2 and an oxide or a salt of an element of group 11 of the periodic table.
专利号:US-9193659-B2 优先权日:2008-02-20 标 题 :Process for the iodination of aromatic compounds 发明人:GIOVENZANA GIOVANNI BATTISTA; CAVALLOTTI CAMILLA; LATTUADA LUCIANO; UGGERI FULVIO 权利人:GIOVENZANA GIOVANNI BATTISTA; CAVALLOTTI CAMILLA; LATTUADA LUCIANO; UGGERI FULVIO; BRACCO IMAGING SPA 摘要:The present invention relates to a process for the preparation of iodinated phenols, —in particular, it relates to a process including the electrochemical iodination of 3,5-disubstituted phenols of formula (1) to the corresponding 3,5-disubstituted-2, 4,6-triiodophenols of formula (2), which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves. Furthermore, the present invention includes the electrochemical iodination of 3, 5- disubstituted anilines of formula (6) to the corresponding 3,5-disubstituted-2,4,6-triiodoanilins of formula (7).
专利号:US-8766003-B2 优先权日:2010-06-10 标题 :Process for the iodination of phenolic derivatives 发明人:CITTERIO ATTILIO; BATTISTINI ELISA; BELNOME DAVIDE; BUONSANTI FEDERICA; LATTUADA LUCIANO; LEONARDI GABRIELLA; UGGERI FULVIO; VIGNALE EVELIN; VISIGALLI MASSIMO 权利人:CITTERIO ATTILIO; BATTISTINI ELISA; BELNOME DAVIDE; BUONSANTI FEDERICA; LATTUADA LUCIANO; LEONARDI GABRIELLA; UGGERI FULVIO; VIGNALE EVELIN; VISIGALLI MASSIMO; BRACCO IMAGING SPA 摘要:The present invention relates to a process for the preparation of iodinated phenols; in particular; it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted phenol compounds to the corresponding 3,5-disubstituted-2,4,6-triiodophenols, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
专利号:US-3553260-A 优先权日:1967-05-29 标 题 :Radiopaque derivatives of alpha-phenoxy-phenylacetic acid 发明人:FELDER ERNST; PITRE DAVIDE 权利人:BRACCO IND CHIMICA SPA 摘要:A - (3 - N-ALKYL-N-ACETYLAMINO-2,4,6-TRIIODOPHENOXY)PHENYLACETIC ACID AND CLOSELY RELATED DERIVATIVES OF THE FORMULA 1,3,5-TRI(I-),2-((R3-PHENYL)-CH(-COOH)-O-),4-(R2-CO- N(-R1)-)BENZENE WHEREIN R1 IS LOWER ALKYL, R2 IS HYDROGEN OR LOWER ALKYL, AND R3 IS HYDROGEN, HALOGEN OR LOWER ALKYL, AND THE PHYSIOLOGICALLY TOLERATED, WATER SOLUBLE METAL OR AMINE SALTS THEREOF ARE RADIOPAQUE, TEND TO ACCUMULATE IN THE GALL BLADDER WHEN APPLIIED ORALLY, AND ARE NON-TOXIC IN EFFECTIVE AMOUNTS. THE CORRESPONDING LOWER ALKYL ESTERS ARE INTERMEDIATES IN THE SYNTHESIS OF THE ACIDS AND SALTS.
专利号:US-12087564-B2 优先权日:2012-05-21 标题 :Tuned synthetic dendrimer calibrants for mass spectrometry 发明人:GRAYSON SCOTT 权利人:THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND 摘要:Provided are synthetic dendrimer calibrants for mass spectrometry. The calibrants are distinguished by their relative case and rapidity of synthesis, comparatively low cost, long shelf life, high purity, and amenability to batch synthesis as mixtures. The latter characteristic enables parallel preparation of higher molecular weight compounds displaying useful distributions of discrete molecular weights, thereby providing multi-point mass spectrometry calibration standards. Methods of making, tuning and using said calibrants are provided.
[参考文献]: Liu S, Et Al. 2,4,6-Triiodophenol Exhibits Embryotoxicity To Pre-Implantation Mouse Embryos In An In Vitro Exposure Model. Ecotoxicol Environ Saf. 2022 Aug;241:113745. [参考文献]: Trocóniz If, Et Al. Dealing With Time-Dependent Pharmacokinetics During The Early Clinical Development Of A New Leukotriene B4 Synthesis Inhibitor. Pharm Res. 2006 Jul;23(7):1533-42. [参考文献]: Craig M Butt, Et Al. Halogenated Phenolic Contaminants Inhibit The In Vitro Activity Of The Thyroid-Regulating Deiodinases In Human Liver. Toxicol Sci. 2011 Dec;124(2):339-47. [参考文献]: G J Miroy, Et Al. Inhibiting Transthyretin Amyloid Fibril Formation Via Protein Stabilization. Proc Natl Acad Sci U S A. 1996 Dec 24;93(26):15051-6. [参考文献]: Iaki F Trocóniz, Et Al. Dealing With Time-Dependent Pharmacokinetics During The Early Clinical Development Of A New Leukotriene B4 Synthesis Inhibitor. Pharm Res. 2006 Jul;23(7):1533-42.
合成参考文献
参考文献:10.1007/s11095-006-0254-1 摘要:Trocóniz IF, Zsolt I, Garrido MJ, Valle M, Antonijoan RM, Barbanoj MJ. Dealing with Time-Dependent Pharmacokinetics during the Early Clinical Development of a New Leukotriene B4 Synthesis Inhibitor. Pharmaceutical Research. 2006 Jun 21;23(7):1533–42. doi: 10.1007/s11095-006-0254-1.