L-2-((三氟甲基磺酰基)氧基)丙酸乙酯置于tetrabutylammonium Fluoride Hydrofluoride体系中,用 二氯甲烷 用作溶剂,化学反应生成2-氟丙酸乙酯 参考文献:Nucleophilic Fluorination Of Triflates By Tetrabutylammonium Bifluoride 标题:Nucleophilic Fluorination Of Triflates By Tetrabutylammonium Bifluoride 摘要:Careful Examination Of Nucleophilicity,Basicity,And Leaving Group Ability Led Us To Discover The Nucleophilic Fluorination Of Triflates By Weakly Basic Tetrabutylammonium Bifluoride,Which Provides Excellent Yields With Minimal Formation Of Elimination-Derived Side Products. Primary Hydroxyl Groups As Well As Secondary Hydroxyl Groups In Acyclic Chains Or In Five-Membered Rings Are Excellent Substrates,Whereas Benzylic And Aldol-Type Secondary Hydroxyl Groups Give Poor Yields As A Result Of The Instability Of Their Triflates. Doi:10.1021/jo8015659
专利号:US-9376410-B2 优先权日:2012-10-10 标题 :(2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone and preparation method and use thereof 发明人:WANG GUAN; JIANG XIANGRUI; GONG XUDONG; CHEN WEIMING; ZHU FUQIANG; ZHANG RONGXIA; ZHAO XIANGUO 权利人:TOPHARMAN SHANGHAI CO LTD; SHANGHAI INST MATERIA MEDICA; TOPHARMAN SHANDONG CO LTD; SHANGHAI INST MATERIA MEDICA 摘要:This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.
参考文献:10.1007/s10924-017-0945-1 摘要:Kundys A, Białecka-Florjańczyk E, Fabiszewska A, Małajowicz J. Candida antarctica Lipase B as Catalyst for Cyclic Esters Synthesis, Their Polymerization and Degradation of Aliphatic Polyesters. Journal of Polymers and the Environment. 2017 Jan 24;26(1):396–407. doi: 10.1007/s10924-017-0945-1.