专利号:US-8748660-B2 优先权日:2012-07-09 标题:Process for the synthesis of antiepileptic drug lacosamide 发明人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD 权利人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD; COUNCIL SCIENT IND RES 摘要:The present invention relates to the improved and efficient process for the synthesis of antiepileptic drug Lacosamide in high enantiopurity (>98% ee) and better yield. More particularly, the present invention relates to improved and efficient, cost effective process for synthesis of desired (R) isomer of Lacosamide starting from commercially available (S)-benzyl glycidyl ether.
专利号:US-9862687-B2 优先权日:2013-11-15 标题:Morphic forms of hexadecyloxypropyl-phosphonate esters and methods of synthesis thereof 发明人:WARE JR ROY WENDELL; DOWNEY AARON LEIGH 权利人:CHIMERIX INC; CHIMERIX INC 摘要:The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.
专利号:US-9303051-B2 优先权日:2010-08-31 标 题 :Phosphonate ester derivatives and methods of synthesis thereof 发明人:WARE ROY W; ALMOND MERRICK R; LAMPERT BERNHARD M 权利人:CHIMERIX INC; CHIMERIX INC 摘要:The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.
专利号:US-9550719-B2 优先权日:2013-05-09 标题 :Process for the preparation of 3-aryl-2-hydroxy propanoic acid compounds 发明人:MURUGAN MUTHUKRISHNAN; MOHAMMAD MUJAHID 权利人:COUNCIL SCIENT IND RES 摘要:The present disclosure provides a process for synthesis of 3-aryl-2-hydroxy propanoic acid derivatives of formula (S)-1. wherein R 1 represents H or (C 1 -C 5 ) alkyl groups and R 2 represents (C 1 -C 5 ) alkyl groups.
专利号:US-6541647-B2 优先权日:1998-07-03 标 题:Methods of synthesis of substituted tetrahydrofuran compound 发明人:CHORGHADE MUKUND SHANKAR; GURJAR MUKUND KESHAO; KRISHNA PALAKODETY RADHA; LALITHA SISTA VENKATA SAI; SADALAPURE KASHINATH; ADHIKARI SUSANTA SEKHAR; MURUGAIAH ANDAPPAN MURUGAIAH S; MHASKAR SUNIL VYANKATESH; SHARMA GANGAVARAM VASANTHA MAD; PRASAD TANGALLAPALLY RAJENDRA; SREENIVAS PUNNA; REDDY VAVILALA GOVERDHAN; ISLAM AMINUL; PRASAD CHITTINENI HARI; RAO ALLA VENKATA RAMA 权利人:MILLENNIUM PHARM INC 摘要:The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1 -butynyl)-tetrahydrofuran and precursors thereof.
专利号:US-9328066-B2 优先权日:2011-05-27 标 题 :Chiral synthesis of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides 发明人:FEY PETER; MAYER AGATHE CHRISTINE 权利人:FEY PETER; MAYER AGATHE CHRISTINE; BAYER IP GMBH 摘要:The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.
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