2-氰基丙烯酸酯類手性衍生物的合成與生物活性研究.pdf

1、貴州大學碩士學位論文2氰基丙烯酸酯類手性衍生物的合成與生物活性研究姓名：張慧蘋申請學位級別：碩士專業(yè)：農(nóng)藥學指導教師：胡德禹宋寶安200606010。!_^0‘、q～搴、芳州大筍2006屆麗壬蒼戈SynthesisandBioactivitiesofNovelChiral2一CyanoacrylatesDerivatives—’Abstract——2Cyanoacrylateisakindofcompoundwithversatileb

2、iologicalactivitiesappliedinagrochemistrywidelyInourpreviousworkaboutsynthesisofcyanoacrylatesincludingpyridylandtrifluoromethylmoiety，thesecompoundswerefoundtopossessmodestanti—TMVactivitiesandantiproliferationactivitie

3、stOPC3cellsforthefirsttimeSoaseriesofnewchiralcompoundstargetedonTMVweredesignedandsynthesizedbyintroducingR)一or(S)一1一phenylethylamineintocyanoacrylateandhopedtoscreencompoundswithhighantivirusactivitiesStartedfromethylc

4、yanoacetate，39titlecompoundsweresynthesizedundermicrowaveirradiation，amongwhich22Werechiralones，Allcompoundswereconfirmedby1HNMR，”CNMR，IRandelementalanalysisThecrystalstructuresofcompoundsIaandllaRwereconfirmedbyX—raydif

5、fractionFromthecrystalstructurewegotthatcompoundsIand11werebothofEisomerXrayintensitydataofIIaRlistedasfollowings：thecrystalbelongstOorthorhombiecrystalsystem，spacegroupisPea21，a209152(3)nm，b=11221(4)nm，c=20691(6)nm，礦=21

6、249(11)nm’，Z=4，Dx=1261g／cm’，A=71073nm，0=206。25010，蘆=0100mm“andF(ooo)=840，thefinalleast—squarescyclegaveR=O0707，wR=0I786，respectivelyApm。=338e／nm’Tooptimizethereactionconditions，thesynthesisof1and11werecarriedoutunderseve

7、ralconditionsTheeffectsofdifferentsolvents，reactiontime，andtheuseofmicrowaveirradiationonthereactionornotwereinvestigatedTheconditionsmoreviableobtained：undermicrowaveirradiationof600Wat50℃for30一45minutes，compounds1weres

8、ynthesizedwithhighyields(640～935％)；andat600W：97“Creactedfor20～30minobtainedcompounds11withyieldsbetween576～823％ComparingwiththedrawbacksoftheclassicalmethodthepresentoneoffersseveraladvantagesincludinggreeneLfasterreacti

9、onrates，fewerbyproducts，andhigheryieldsThetitlecompoundswereevaluatedforherbicidal，anticancerandanti—TMVactivitiesAndtheresultsofbioassayshowedthat：compoundsdesigneddidnotshowherbicidalactivitybutpossessedpromisingactivi