专利号:WO-2005051933-A1 优先权日:2003-11-28 标题 :An improved process for the synthesis of 4-(4-benzyloxy-carbonylamino-2-fluorophenyl)-piperazine-1-carboxylic acid tert-butyl ester, a key intermediate for oxazolidinone antimicrobials and compounds prepared thereby 发明人:KUMAR YATENDRA; KAUL VIJAY KUMAR; SINGH NITU; YADAV GYAN CHAND 权利人:RANBAXY LAB LTD; KUMAR YATENDRA; KAUL VIJAY KUMAR; SINGH NITU; YADAV GYAN CHAND 摘要:Provided herein are process for the synthesis of the 4-(4-benzyloxy-carbonylamino-2-fluorophenyl)-piperazine-1-carboxylic acid tert-butyl ester, which is a key intermediate in the synthesis of oxazolidinone compounds having antibacterial activity. Also provided herein are processes for preparing oxazolidinone compounds. In addition, compounds prepared by the processes provided herein are also encompassed. Formula (I) and Formula (II).
专利号:US-5354439-A 优先权日:1990-07-16 标 题 :Process for the synthesis of fluorinated derivatives 发明人:FORAT GERARD; GILBERT LAURENT; LANGLOIS BERNARD 权利人:RHONE POULENC CHIMIE 摘要:A process for the synthesis of fluorinated organic compounds and a reagent suitable for use in the process. The process is carried out by exchange with fluorides, while preferably agitating the reaction medium with ultrasonic sound.
专利号:US-2022315594-A1 优先权日:2019-08-09 标 题 :Method of synthesis of compound for dual inhibition of jak2 and bet 发明人:UPADHAYAYA RAM SHANKAR; UKKALAM MURALI KRISHNA; SARMA K NARASIMHA 权利人:OHM ONCOLOGY 摘要:Embodiments of the invention include quinoline compounds and methods of synthesis. Ohm-581 has demonstrated dual inhibition of JAK2 and BET and acts as a therapeutic agent for micosis fungoides (MF) and other hematologic malignancies. Embodiments also include an efficient process for the preparation of Ohm-581 and pharmaceutically acceptable salts. The process is suited for large-scale production of quinoline compounds including Ohm-581.
专利号:US-9233989-B2 优先权日:2011-10-11 标题:Sila analogs of oxazolidinone derivatives and synthesis thereof 发明人:REDDY DUMBALA SRINIVASA; BALAMKUNDU SEETHARAM SINGH; RAMESH REMYA 权利人:COUNCIL SCIENT IND RES 摘要:The invention discloses silaanalogs of oxazolidinone compounds, to pharmaceutical compositions and to the synthesis of the oxazolidinone derivatives of formula I. The invention further relates to methods of treating a subject suffering with gram positive pathogens including those resistant to methicillin and vancomycin using the compound(s) or modulation of coagulation properties of blood-clotting cascade or compositions of the oxazolidinone derivatives of the invention.
专利号:US-6448449-B2 优先权日:2000-04-21 标题:Process for preparation of (R)-1- (aryloxy)propan-2-ol 发明人:LARROW JAY FRANCIS 权利人:RHODIA CHIREX INC 摘要:A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol, which is a useful intermediate in the synthesis of the widely used antibiotic Levofloxacin is provided. A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-2-trimethylsiloxypropane is also described. The process includes the ring opening of (R)-propylene oxide with 2,3-difluoro-6-nitrophenyl trimethylsilyl ether in the presence of an optically active Co(salen) catalyst. The trimethylsilyl group of the reactant is transferred to the product aryloxy alcohol, which serves to protect the secondary alcohol in situ. Upon isolation, the trimethylsilyl group is removed and the resulting regioisomeric mixture purified to yield the desired (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol in high purity and yield.
专利号:US-2010286211-A1 优先权日:2004-10-08 标题:Oxazolidinone derivatives as antimicrobials 发明人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 权利人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 119. 摘要:Sakya, S. M.; Yang, J., Science of Synthesis Knowledge Updates, (2012) 1, 227.