合成目标产物 Cefditoren Pivoxil 主要起始原料 Iodomethyl Pivalate And Cefditoren
(文献来源)合成步骤主要原料 Iodomethyl Pivalate 和 Cefditoren
7-苯乙酰氨基-3-氯甲基-4-头孢烷酸对甲氧基苄酯置于吡啶,甲醇,碳酸氢钠,苯甲醚,三氟乙酸,Sodium Iodide,三氯氧磷体系中,用 二氯甲烷,水,N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 28.0H,反应生成头孢妥仑匹酯 参考文献:Synthesis And Oral Activity Of Pivaloyloxymethyl 7-((Z)-2-(2-Aminothiazol-4-yl)-2-Methoxyiminoacetamido)-3(Z)-(4-Methylthiazol-5-yl)Vinyl-3-Cephem-4-Carboxylate(Me1207) And Its Related Compound. 标题:Synthesis And Oral Activity Of Pivaloyloxymethyl 7-((Z)-2-(2-Aminothiazol-4-yl)-2-Methoxyiminoacetamido)-3(Z)-(4-Methylthiazol-5-yl)Vinyl-3-Cephem-4-Carboxylate(Me1207) And Its Related Compound. 摘要:7-[2-(2-氨基噻唑-4-基)-2(Z)-甲氧亚胺乙酰氨基]-3(Z)-(4-甲基噻唑-5-基)乙烯-3-头孢烯-4-羧酸(11,Me1206)及其3-Trans异构体(13)被制备用于测试抗菌活性.这些化合物对革兰氏阳性菌和革兰氏阴性菌均表现出优秀的抗菌活性,包括 β-内酰胺酶产生菌株.通过与酰基碘代匹伐酸酯酯化反应,制备了这些化合物(11和13)的匹伐酸氧甲基酯(12和14).其中,匹伐酸氧甲基 7-[(Z)-2-(2-氨基噻唑-4-基)-2-甲氧亚胺乙酰氨基]-3(Z)-(4-甲基噻唑-5-基)乙烯-3-头孢烯-4-羧酸酯(12,Me1207)在小鼠口服给药后显示出非常好的尿液回收率. Doi:10.1248/cpb.39.2433
专利号:US-2024197774-A1 优先权日:2021-04-16 标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles 发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO 权利人:UNIV TEXAS 摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.
专利号:WO-2005100367-A1 优先权日:2004-04-13 标 题 :Intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins 发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH KAPTAN; PRASAD ASHOK; RICHHARIYA SANTOSH 权利人:RANBAXY LAB LTD; KUMAR YATENDRA; PRASAD MOHAN; SINGH KAPTAN; PRASAD ASHOK; RICHHARIYA SANTOSH 摘要:The present invention relates to crystalline intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins and processes for their preparation. In particular, the present invention relates to crystalline ylides of Formula I, processes for their preparation, and their use as an intermediate in thepreparation of 3-(2-substituted vinyl) cephalosporins.
专利号:US-7452990-B2 优先权日:2002-12-26 标题 :Intermediates for synthesis of cephalosporins and process for preparation of such intermediates 发明人:DATTA DEBASHISH; DANTU MURALIKRISHNA; MISHRA BRIJKISHORE; SHARMA POLLEPEDDI LAKSHMI NARAYANA 权利人:LUPIN LTD 摘要:A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics n nwhereinn n X is chlorine or bromine; R is hydrogen, C 1-4 alkyl group, an easily removable hydroxyl protective group, —CH 2 COOR 5 , or —C(CH 3 ) 2 COOR 5 , wherein R 5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV 1 ), n nwherein X, R and R 5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII)n n nin an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.
专利号:US-10947203-B2 优先权日:2016-03-25 标题 :1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor 发明人:CHEN TAOSHENG; LIN WENWEI; WANG YUEMING 权利人:ST JUDE CHILDRENS RES HOSPITAL; ST JUDE CHILDRENS RSEARCH HOSPITAL 摘要:In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: n nwhich are modulators the pregnane X receptor (“PXRâ€?); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-9879050-B2 优先权日:2013-08-30 标 题 :Substituted urea depsipeptide analogs as activators of the CLPP endopeptidase 发明人:LEE RICHARD E; ZHAO YING; GRIFFITH ELIZABETH; ZHENG ZHONG; SINGH AMAN P 权利人:ST JUDE CHILDREN'S RES HOSPITAL 摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-2006135761-A1 优先权日:2002-12-26 标 题 :Novel intermediates for synthesis of cephalosporins and process for preparation of such intermediates