📜Ethyl 2-<2,3,5-Trifluoro-4-(4-Methyl-1-Piperazinyl)-Benzoyl>-3-Dimethylaminoacrylate置于sodium Hydroxide,Sodium Hydride体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应 20.25H,反应生成盐酸芦氟沙星 参考文献:One-Pot Synthesis Of Rufloxacin 标题:One-Pot Synthesis Of Rufloxacin 摘要:Rufloxacin (Mf-934) Was Prepared In One-Pot Synthesis In 61% Yield By Treatment Of The 2,3,5-Trifluoro-4-(4-Methyl-1-Piperazinyl)-Benzoyl Acetate,First With N,N-Dimethylformamide Dimethyl Acetal,Then With 2-Aminoethanethiol,Followed By Cyclization And Hydrolysis. Doi:10.1080/00397919108021589
专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:WO-2015183067-A1 优先权日:2014-05-30 标题 :Synthesis of analogues of y-amino acids and resulting products 发明人:FERNÃ?NDEZ ZERTUCHE MARIO; TOVAR GUDIÑO ERIKA; TRUJILLO FERRARA JOSÉ GUADALUPE; GUEVARA SALAZAR JUAN ALBERTO 权利人:UNIV AUTÓNOMA DEL ESTADO DE MORELOS 摘要:The invention relates to a compound of formula (see formula), suitable for use as drugs in the treatment of chronic neurodegenerative disorders of the Huntington's disease, Parkinson's disease and epilepsy type, inter alia . The invention relates to novel methods for the synthesis of said analogues and the pharmaceutically acceptable solvates and salts thereof.
专利号:US-2023398527-A1 优先权日:2020-10-15 标 题 :Acridinium-based photoredox catalysts, synthesis and use thereof in oxidative cleavage of c-o bonds 发明人:SOULÉ JEAN-FRANÇOIS 权利人:UNIV RENNES; CENTRE NAT RECH SCIENT; ECOLE NAT SUPERIEURE DE CHIMIE; INSTITUT NAT DES SCIENCES APPLIQUEES DE RENNES 摘要:The present invention belongs to the field of catalytic chemistry, and more specifically to catalysed oxidation of lignin. It also relates to synthesis of catalyst compounds. n The present invention relates to new acridinium-based photoredox catalyst compounds and their use thereof in a chemical reaction, preferably in depolymerisation of lignin models and ultimately lignin. The invention also relates to the method of synthesis of the new acridinium-based photoredox catalyst compounds according to the invention.
专利号:US-6699981-B2 优先权日:1999-09-22 标题 :Method and compositions for improved polynucleotide synthesis 发明人:YANG SHUWEI 权利人:GENECOPOEIA INC 摘要:The sensitivity and specificity of polynucleotide synthesis is increased by protecting the 3'-end of an oligonucleotide used as a primer in the synthesis of the polynucleotide. Protection of the 3'-end of an oligonucleotide prevents non-specific chain elongation. Removal of blocking group an elevated temperature, using a thermostable enzyme, permits template-specific polynucleotide synthesis. The present invention also provides oligonucleotides with a 3' end protected by a blocking group and a thermostable enzyme capable of removing the blocking group at an elevated temperature. The compositions and methods of the invention are very useful in a variety of techniques for DNA/RNA amplification and analysis, including medical genetics research and diagnosis, pathogen detection, forensic, and animal and plant genetics applications, among others.
专利号:WO-2006025724-A1 优先权日:2004-09-02 标题:IMPROVEMENTS TO SYNTHESIS, PHARMACEUTICAL COMPOSITIONS AND USES OF SODIUM PENTABORATE PENTAHYDRATE (NaB5O8.5H2O) 发明人:GALVAN PEREZ JUAN PABLO 权利人:GALVAN PEREZ JUAN PABLO 摘要:The invention relates to an improved method for the synthesis of sodium pentaborate pentahydrate (NaB5O8.5H2O), consisting in reacting disodium tetraborate decahydrate (DTBD, Borax) and orthoboric acid (OBA, boric acid). The inventive method is performed over a period of no more than five days and does not require the use of fungal strains. The invention also relates to the product thus obtained, which is intended to boost the immune system against ailments caused by bacteria and viruses, to the pharmaceutical compositions thereof and to the use of same in relation to said ailments.
专利号:US-5888775-A 优先权日:1994-04-29 标题:Peptide synthesis and purification by fusion to penI protein or precipitation effective portion thereof 发明人:TAL RONY; WONG HING C; CASIPIT CLAYTON; CHAVAILLAZ PIERRE-ANDRE; WITTMAN VAUGHAN 权利人:DADE INT INC 摘要:The present invention provides novel methods for the synthesis and isolation and purification of a peptide of interest (target peptide). In particular, the invention relates to peptide synthesis, isolation and purification methods that comprise use of penI fusion polypeptides and related gene fusion constructs that encode such polypeptides.
1. Piddock, L.J.V., Panchal, S., and Norte, V. Comparison of the mechanism of action and resistance of two new fluoroquinolones, rufloxacin and MF961 with those of ofloxacin and fleroxacin in Gram-negative and Gram-positive bacteria. J. Antimicrob. Chemother. 31(6), 855-863 (1993). 2. Cecchetti, V., Fravolini, A., Fringuelli, R., et al. Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids. J. Med. Chem. 30(3), 465-473 (1987). 3. Fabbri, S., Broggini, M., Pagella, P., et al. The inhibition of supercoiling activity of DNA gyrase from Micrococcus luteus caused by rufloxacin (MF 934) and MF 961. J. Antimicrob. Chemother. 27(5), 687-689 (1991). 4. Bonina, L., Carbone, M., Mastroeni, P., et al. Effects of rufloxacin in Salmonella typhimurium infection in mice. J. Chemother. 4(6), 353-357 (1992). 5: Burgalassi S, Cappello B, Chetoni P, Iervolino M, Monti D, Saettone MF. Rufloxacin eyedrops: effect of different formulations on ocular pharmacokinetics in rabbits. Eur J Ophthalmol. 2006 Mar-Apr;16(2):311-7. doi: 10.1177/112067210601600219. 28(6):1161-71. doi: 10.1016/s0731-7085(02)00054-7.
合成参考文献
参考文献:10.2165/11587280-000000000-00000 摘要:Tomé AM, Filipe A. Quinolones: review of psychiatric and neurological adverse reactions. Drug Saf. 2011 Jun 01;34(6):465–88. doi: 10.2165/11587280-000000000-00000. 参考文献:10.2165/00003495-199958002-00001 摘要:Andriole VT. The future of the quinolones. Drugs. 1999;58 Suppl 2():1–5. doi: 10.2165/00003495-199958002-00001. 参考文献:10.2165/00003495-199958002-00005 摘要:Eliopoulos GM. Activity of newer fluoroquinolones in vitro against gram-positive bacteria. Drugs. 1999;58 Suppl 2():23–8. doi: 10.2165/00003495-199958002-00005. 参考文献:10.2165/00003495-199958002-00006 摘要:Turnidge J. Pharmacokinetics and pharmacodynamics of fluoroquinolones. Drugs. 1999;58 Suppl 2():29–36. doi: 10.2165/00003495-199958002-00006. 参考文献:10.2165/00003495-199958002-00013 摘要:Edlund C, Nord CE. Effect of quinolones on intestinal ecology. Drugs. 1999;58 Suppl 2():65–70. doi: 10.2165/00003495-199958002-00013.