功能單體的酶催化選擇性合成研究.pdf

1、英文題名：旦墜圣Y墊叢i魚5星!曼堡!iY曼Y墮魚星s地Q￡魚墮壘!iQ衛(wèi)旦!塑Q塾Qm曼!博士后姓名：昱起流動嗷■級學(xué)袖名稱：撾料型堂皇王猩專業(yè)(二級學(xué)科)名稱：撾料絲堂合作教授姓名：撻賢塑研究工作起始時間：2QQ3生壘旦研究工作期滿時間：2QQ三生壘旦提交報告日期：2QQ三生3旦————————竺竺竺塑竺竺竺生————一⑧—_—————√——————————————————————?！?。———————

2、———‘?！薄病甞‘。鮒AbstractSynthesisofpolymerizabledrugderiVanvesisoneofuleimportantresearchfieldsinmepolymericdmgsGenerally，drugmoIeculescomainmallyactiVegroupsEnzymaticsyn也esisjsane丘bctivemethodwithhi曲selectivityf

3、orthesynthesisof^mctionalmonomerThisreportfocusesone11zymaticselectivesynthesisofpolym甜zable2’一deox”lridine，phytomeljn，c”arabine，acyclovira11dcyclodextrinvinylestersinnon—aqueousmediaAseriesoffunctionalmonomerswitlldifI’

4、erentacylationpositionwerepreparedandcha麟terizedby‘HNMR，”CNMR，F(xiàn)TlRandESl一MSWfindthattheenzvmaticselectiVitycanbeadjuSted卸dcon訂olledbythechan西ngofmereactionconditions(1)Intheegterificationof2’一deoxy砸diⅡe，Lipozymeinacetone

5、sbowedhi幽regioselectiVeactiV時towardthe5’primaryhydroxyl，andindioxidetoward3’secondafyhydroxylof2’dcox”ridinePPLinacetoneandTHFalsoshowedhighregioselectiveactivitytoward3’secondaryhy出oxyl(2)Intlleesterificationofph”omelin

6、，alkalineprotease行om正踣cfⅣ甜sJ“6r玎括inp州dineshowedlli曲regioselectivitytoward恤3”hydmxyIofph”omelin，whileinbutylalcoholNoVozym435selectiVelyacylatedme4’’’hydroxylofph”omelin(3)Intheester湎cationofcytarabinc，alkalineproteasefmm

7、點婦cfZ如村s“6fj凰inpvridineca乜lyzedtheacyl砸onofc—s’hydroxylandC一4蕊n0group，meyieldsis54％a11d23％，respectiVelyInacetoneL印ozym。Showedhighregiosele“v時towardthec一5’hydroxylofcytarabine，、v：hiletlleyieldsislowaIldtllereactionneed如rt

8、heroptimizationUsingchemicalm劬odindioxanethemainproductisthederiV撕veacylatedatC一4撇inogroup(4)Intheesterifica廿onofacyclov址alkalineproteasefrom肋cf口淞占“6“凰inpyridinecatalyzedtheacylationofC一8hydmxyI，howcv盯，sodiummethoxideinD

9、MFcangivetheacylationproductofC—laIni芏logroup(5)Transesterificationofcyclodextrin(B—CD)、)lritllthreedivinyIdicarboxylatesandfivefa仕yacidvinyIesters，cat出zedby岫alkalineproteasefromBacmussubtilisinanhydrousDMF，如mishedmeco眥s