4,6-二氯嘧啶置于溶剂黄146体系中,用 Sodium Hydroxide 用作溶剂,以99%的收率获得2-氨基-6-氯-4-羟基嘧啶 参考文献:Novel Intermediates For The Preparation Of Carbovir 标题:Novel Intermediates For The Preparation Of Carbovir 摘要:该发明提供了一种新型的环戊烯基醇化合物,可用作制备抗艾滋病药物卡波韦的中间体.还提供了制备这种新型化合物以及利用这些化合物制备卡波韦的方法.
专利信息
专利号:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
专利号:WO-2012127472-A1 优先权日:2011-03-22 标题:Process and intermediates for the preparation of preladenant and related compounds 发明人:MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI 权利人:MAPI PHARMA LTD; MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI 摘要:The present invention describes processes for the synthesis of 2-(furan-2-yl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-l-yl] ethyl]-7H-pyrazolo[ 4,3-e ][1,2,4]- triazolo[1,5c] pyrimidin-5-amine (Preladenant) represented by the structure of formula (1 ), and solvates and salts thereof, especially salts with pharmaceutically acceptable acids. The process of the present invention is useful not only for Preladenant production, but also for the preparation of other biologically active compounds of general formula (17), such as A2a receptor antagonists used for the treatment of central nervous system diseases, among others. The present invention further relates to certain intermediates formed in such processes.
专利号:US-2005085492-A1 优先权日:2003-10-20 标 题:Stereoselective process for the synthesis of chiral garft compounds and intermediates 发明人:RAHMAN LEERA 权利人:AGOURON PHARMACEUTICALS MINC 摘要:The present invention describes a stereoselective preparation of derivatives and precursors of molecules having formula 1: n nMethod of preparing the compounds, intermediates and derivatives are described. The methods described herein allow the preparation of diastereomeric forms of compound having formula 1. The compounds of the invention are GARFT inhibitors.
专利号:US-3959278-A 优先权日:1970-07-27 标 题 :Method of synthesis of pteridines 发明人:WOOD HAMISH CHRISTOPHER SWAN; STUART ALEXANDER; CURRAN ADRIAN CHARLES WARD; AL-HASSAN SAIEBA 权利人:BURROUGHS WELLCOME CO 摘要:A pharmaceutical formulation of a compound of formula (II') ##SPC1## n wherein Y is a lower alkyl group, in association with a pharmaceutically acceptable carrier, as an antibacterial product, and methods involving the preparation and reductive cyclization of a compound of formula (IV) ##SPC2## n wherein X is a lower alkyl group or a hydroxymethyl group.
专利号:US-5401844-A 优先权日:1983-04-11 标 题 :Regulation of enzymes which utilize tetrahydrobiopterin or tetrahydrofolate cofactors with 6,6-disubstituted-tetrahydropteridines 发明人:AYLING JUNE E; BAILEY STEVEN W 权利人:UNIV SOUTH ALABAMA 摘要:6-[2'-Amino-2',2'-disubstituted-ethylamino]-pyrimidines of the structure: ##STR1## in which X=H, NH 2 or NO 2 , which are novel intermediates in the synthesis of quinoid 6,6-disubstituted-dihydro- and 6,6-disubstituted-tetrahydro-pteridines, are claimed.
专利号:US-11912734-B2 优先权日:2020-01-28 标题:Solid-phase synthesis of oligonucleotides containing N6-(2-deoxy-alpha,beta-derythropentofuranosyl)-2,6-diamino-4-hydroxy-5-formamidopyrimidine (Fapyâ‹…dG) 发明人:GREENBERG MARC M; YANG HAOZHE 权利人:UNIV JOHNS HOPKINS 摘要:A strategy using reverse phosphoramidites for synthesizing oligonucleotides containing Fapy·dG is disclosed.
参考标题:The Synthesis Of 7-Deazaguanines As Potential Inhibitors Of Guanosine Triphosphate Cyclohydrolase I 作者:Colin L Gibson,Salvatore La Rosa,Kyuji Ohta,Peter H Boyle,Fabien Leurquin,Alexandra Lemaçon,Colin J Suckling |发布日期:2004.1 摘要:Compounds Can Be Prepared. These Methods Supplement Our Previous Work That Established Routes For The Synthesis Of 7- And 8-Substituted 7-Deazaguanines. Emphasis Is Placed On The Properties Of 2-Thioalkyl Pyrimidines As Intermediates Because They Provide The Basis For A Traceless Solid-State Synthesis Of Purines, Pteridines, And Their Analogues. Compounds Prepared Have Been Assessed In A Primary Screen For
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 335. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 459. 摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#02771 摘要:I. Wempen and J.J. Fox. J. Med. Chem. 6, 688 (1963).