(S)-1,3-Dichloro-1-Propanol置于氢氧化钾体系中,用 甲醇 作为反应溶剂,以51%的收率获得产物右旋环氧氯丙烷 参考文献:Preparative Production Of Optically Active Esters And Alcohols Using Esterase-Catalyzed Stereospecific Transesterification In Organic Media 标题:Preparative Production Of Optically Active Esters And Alcohols Using Esterase-Catalyzed Stereospecific Transesterification In Organic Media 摘要: DOI:10.1021/ja00321A033
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-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:WO-2013046211-A1 优先权日:2011-09-27 标 题 :Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl) phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide and intermediates thereof 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 摘要:TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.
专利号:US-10647672-B2 优先权日:2017-10-03 标 题:Modulators of cell adhesion, methods and compositions therefor 发明人:BLASCHUK OREST WILLIAM 权利人:Zonula Incorporated; ZONULA INC 摘要:Compounds with activity as modulators of cell adhesion are disclosed. The compounds are derivatives of piperidin-4-amine. In some embodiments, a compound can be linked to a targeting agent, a pharmaceutically active substance and/or a support material. Methods for enhancing or inhibiting classical cadherin-mediated functions are also disclosed. The compounds can be used for the treatment or prevention of a variety of diseases including cancer. Compositions and devices, including skin patches comprising a compound are also disclosed. In addition, methods of synthesis of the compounds are provided.
专利号:EP-2397141-A1 优先权日:2010-06-16 标 题:Process for the synthesis of beta-amino acids and derivatives thereof 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to a process for the preparation of β-amino acids and derivatives thereof, which is especially suited for gliptins and particularly sitagliptin. A key step makes use of suitably derivatized epoxides or aziridines, which owing to a chirality provides a source of chirality for intermediates which are suitable for building up β-amino acids and similar compounds, in particular in the construction of the sitagliptin molecule.
专利号:WO-2006031179-A1 优先权日:2004-09-13 标 题:Process for preparation of phtalimide 发明人:KRIG ANN-SOFIE; THELIN MATS 权利人:ASTRAZENECA AB; KRIG ANN-SOFIE; THELIN MATS 摘要:The present invention is directed to a novel process for the synthesis of (S) -glycidyl phthalimide and to novel intermediates in the process. The process comprises, reacting a (R) -3 -Chloro-1,2-propanediol and phtalimide salt. Then reacting the product with trimethylorthoacetate and an essentially water free acid. Then reacting the product with acetyl halogenide and do a basic ester hydrolysis.
参考文献:10.4061/2011/982854 摘要:New N, Mohandas J, John GT, Ratanjee S, Healy H, Francis L, Ranganathan D. Calcific Uremic Arteriolopathy in Peritoneal Dialysis Populations. International Journal of Nephrology. 2011;2011():1–9. doi: 10.4061/2011/982854. 摘要:Draca N, Tikvica A, Eljuga D, Semenski D, Brncić M, Vukicević S. Biomechanical properties of bones from rats treated with sevelamer. Coll Antropol. 2011 Jun;35(2):557–63. 参考文献:10.1097/rhu.0b013e3182288acd 摘要:Akasbi N, Houssaini TS, Rabhi S, Lahlou M, Boukhrissa A, Tahiri L, El Maaroufi C, Berrady R, Harzy T, Bono W. Diffuse uremic tumoral calcinosis in a patient on long-term hemodialysis. J Clin Rheumatol. 2011 Aug;17(5):272–4. doi: 10.1097/rhu.0b013e3182288acd.