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:EP-0438796-B1 优先权日:1990-01-22 标题:Process for the enantioselection synthesis of alkylated oxindoles used as intermediates in the preparation of physostigmine 发明人:LEE THOMAS BING KIN DR; WONG GEORGE S K 权利人:HOECHST MARION ROUSSEL INC 摘要:A process for the stereoselective synthesis of [R]- and [S]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-indole-3-acetonitriles comprises reacting racemic and 5-alkoxy-substituted (+/-)-1,3-dimethyloxindoles with a halogenated acetonitrile in the presence of a substituted N-benzyl cinchoninium, quinidinium, cinchonidinium, or quininium catalyst. The resulting alkylated oxindoles can be converted to primary amines by catalytic reduction in the presence of hydrogen gas. One of the primary amines, such as enantiomers of 3-(2-aminoethyl)-1,3-dihydro-1,3-dimethyl-5-methoxy-2H-indol-2-one, can be enriched by contact with a chiral tartaric acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The product can be used in the synthesis of stereospecific forms of physostigmine and related compounds having pharmaceutical activity.
专利号:US-9284306-B2 优先权日:2012-05-11 标题 :(R)-Nifuratel, its use for the treatment of infections and synthesis of (R) and (S)-Nifuratel 发明人:GAGLIARDI STEFANIA; CONSONNI ALESSANDRA; MAILLAND FEDERICO; BULGHERONI ANNA 权利人:POLICHEM SA 摘要:(R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-2006089405-A1 优先权日:2004-10-21 标 题 :Asymmetric synthesis of dihydrobenzofuran derivatives 发明人:ZHOU DAHUI; STACK GARY P; GONTCHAROV ALEXANDER V 权利人:WYETH CORP 摘要:This invention concerns a process for the preparation of benzofuran derivatives. In some aspects, these compounds are of formula I: n n nwherein each of R 1 , R 2 , R 3 , and R 4 is as defined herein.
专利号:US-7439364-B2 优先权日:2001-05-17 标 题 :Process for the synthesis of derivatives of halo-[2,3-F] quinoline 发明人:CHAN ANITA W; CURRAN TIMOTHY T; IERA SILVIO; CHEW WARREN; SELLSTEDT JOHN H; VID GALINA; FEIGELSON GREG; DING ZHIXIAN 权利人:WYETH CORP 摘要:Methods of preparing compounds of Formula I n nare provided.
[参考文献]: Neeraj Bala, Et Al. Bioresolution Of Benzyl Glycidyl Ether Using Whole Cells Of Bacillus Alcalophilus. J Basic Microbiol. 2012 Aug;52(4):383-9. [参考文献]: Rocío Marcos, Et Al. Metal-Mediated Cyclization Of Aryl And Benzyl Glycidyl Ethers: A Complete Scenario. J Am Chem Soc. 2008 Dec 17;130(50):16838-9.
合成参考文献
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