聚合甲醛,利福霉素,1-氨基-4-环戊基哌嗪置于叔丁胺,溶剂黄146体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 利福喷丁 参考文献:Method For Obtaining Rifapentine With A New Crystalline Form 标题:Method For Obtaining Rifapentine With A New Crystalline Form 摘要:A New Crystalline Form Of Rifapentine,The Characterization Thereof And A Method For Obtaining Same Is Disclosed. The Method For Obtaining The New Crystalline Form Includes The Steps Of Adding A Mixture Of Dimethylformamide,Tert-Butylamine And Paraformaldehyde To Rifamycin S In The Presence Of Glacial Acetic Acid; Adding Paraformaldehyde And Heating; Subsequently Adding 1-Amino-4-Cyclopentylpiperazine To Dimethylformamide; Adding Ascorbic Acid To Water; And Mixing,Filtering And Washing The Product The Yield Of Raw Rifapentine Is 87+5% With 99.00% Purity.
专利信息
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:US-2011087037-A1 优先权日:2007-10-31 标题:Synthesis of ring b abeo-sterols as novel inhibitors of mycobacterium tuberculosis 发明人:RODRIGUEZ-PIERLUISSI ABIMAEL D; WEI XIAOMEI 权利人:INTELLECTUAL PROPERTY AND TECHNOLOGY VIC OFF OF 摘要:Novel 3β-hydroxy-Δ 5 -steroid analogs possessing a contracted cyclopentane B-ring provide good inhibitory activity against Mycobacterium tuberculosis . The 5(6→7)abeo-sterol nucleus present in compounds of the invention represents a novel scaffold for the development of new antitubercular agents.
专利号:US-11744867-B2 优先权日:2017-02-14 标 题 :Modulation of microbial synthesis of 4-ethylphenol and 4-ethylphenyl sulfate in behavior and disease 发明人:NEEDHAM BRITTANY D; MAZMANIAN SARKIS K; SHARON GIL; FUNABASHI MASANORI; FISCHBACH MICHAEL A; HSIAO ELAINE Y; PATTERSON PAUL H 权利人:CALIFORNIA INST OF TECHN; UNIV CALIFORNIA 摘要:Some embodiments relate to genetically engineered bacterial strains for modulation of levels of the bacterial metabolite 4-ethylphenol (4EP) and its sulfated form, 4-ethylphenyl sulfate (4EPS). In some embodiments, the bacteria reduce or inhibit production of 4EP or 4EPS in the gut of a subject. The bacteria can ameliorate, delay the onset, or reduce the likelihood of one or more symptoms associated with anxiety and/or autism spectrum disorder (ASD) in the subject.
专利号:US-11851651-B2 优先权日:2017-06-19 标 题 :Automated methods for scalable, parallelized enzymatic biopolymer synthesis and modification using microfluidic devices 发明人:BANAL JAMES; BERLEANT JOSEPH DON; SHEPHERD TYSON; BATHE MARK 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Methods for the automated template-free synthesis of user-defined sequence controlled biopolymers using microfluidic devices are described. The methods facilitate simultaneous synthesis of up to thousands of uniquely addressed biopolymers from the controlled movement and combination of regents as fluid droplets using microfluidic and EWOD-based systems. In some forms, biopolymers including nucleic acids, peptides, carbohydrates, and lipids are synthesized from step-wise assembly of building blocks based on a user-defined sequence of droplet movements. In some forms, the methods synthesize uniquely addressed nucleic acids of up to 1,000 nucleotides in length. Methods for adding, removing and changing barcodes on biopolymers are also provided. Biopolymers synthesized according to the methods, and libraries and databases thereof are also described. Modified biopolymers, including chemically modified nucleotides and biopolymers conjugated to other molecules are described.
专利号:US-10899773-B2 优先权日:2014-12-19 标 题 :Total synthesis of trioxacarcin DC-45-A2 and preparation of trioxacarcin analogs 发明人:NICOLAOU KYRIACOS C; CAI QUAN 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
1: Dorman SE, Savic RM, Goldberg S, Stout JE, Schluger N, Muzanyi G, Johnson JL, Nahid P, Hecker EJ, Heilig CM, Bozeman L, Feng PJ, Moro RN, MacKenzie W, Dooley KE, Nuermberger EL, Vernon A, Weiner M; Tuberculosis Trials Consortium. Daily rifapentine for treatment of pulmonary tuberculosis. A randomized, dose-ranging trial. Am J Respir Crit Care Med. 2015 Feb 1;191(3):333-43. doi: 10.1164/rccm.201410-1843OC. Erratum in: Am J Respir Crit Care Med. 2015 May 15;191(10):1210. 2: Winter H, Egizi E, Murray S, Erondu N, Ginsberg A, Rouse DJ, Severynse-Stevens D, Pauli E. Evaluation of the pharmacokinetic interaction between repeated doses of rifapentine or rifampin and a single dose of bedaquiline in healthy adult subjects. Antimicrob Agents Chemother. 2015 Feb;59(2):1219-24. doi: 10.1128/AAC.04171-14. Epub 2014 Dec 15. 3: Weiner M, Egelund EF, Engle M, Kiser M, Prihoda TJ, Gelfond JA, Mac Kenzie W, Peloquin CA. Pharmacokinetic interaction of rifapentine and raltegravir in healthy volunteers. J Antimicrob Chemother. 2014 Apr;69(4):1079-85. doi: 10.1093/jac/dkt483. Epub 2013 Dec 15.
合成参考文献
摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956