生物可降解peg化喜樹堿前藥及其衍生物的合成

1、V了麗測分類號：墅4：4密級單位代碼：】Q呈9學(xué)號：邀!窆豎塾!壘∞82舍肥工學(xué)大警HefeiUniversityofTechnology碩士學(xué)位論文MASTERDISSERTATIoN論文題目：生物可降解PEG化喜樹堿前藥及其衍生物的合成SyntheseofbiodegradabIepolyethyleneglycol(PEG)linkCamptothecinandderivates學(xué)位類別：堂迓亟學(xué)科專業(yè)：(工程領(lǐng)域)廛旦絲堂作者姓

2、名：秦燕軍導(dǎo)師姓名：縫旦生夔堡完成時間：2007年5月SyntheseofbiodegradabIepolyethyleneglycol(PEG)linkCamptothecinandderivatesABSTRACTThepolymerpro—drugsofeamptotheeinanditsderivatewerepreparedusingSuccinicAnhydrideasalinkspaceinthispaperTheeste

3、rof20一OHenhancesthestabilityoflactone，andtheproductionhasthecharacteristicofslow—releaseandcontrolledreleaseA、Poly(polyethyleneglycolsuccinate)linkedwithesterbondwaspreparedfromPEGandSuccinicAnhydridewith4dimethylaminopy

4、ridineasthecatalystat60“(2TheEffectsofcatalyst，reactiontimeandmolecularweightofPEGonreactionwerestudiedTheresultshowedthatthecatalyticeffectoftriethylamineandpyridinewasinsignificant，whilethecatalyticeffectof4dimethylami

5、nopyridinewassignificant；viscosityaveragemolecularweight(瓦)increasedastimegoneandtheincreasevalueof瓦wasn’tsignificantafter36h；the_oftheproductionpreparedfromPEGwithdifferentmolecularweightwereall40104approximatelyTheresu

6、ltindicatedthatthePoly(polyethyleneglycolsuccinate)wasdegradableatphysiologicalconditionpH、pigpancreaticlipaseandpapain，andthatPoIy(polyethyleneglycolsuccinate)withahigherportionofesterbondshowedhigherdegradationrateBiod

7、egradablepolyethyleneglycol(PEG)link—CamptothecinwaspreparefromPoly(polyethyleneglycolsuccinate)andCampptothecinSuccinicAnhydridewithdieyclohexylcarbodiimideasadehydratingagent。B、CampptothecinSuccinicAnhydridewasprepaedf

8、romcamptothecinandsuccinicadhydridewith4dimethylaminopyridineasthecatalystat40“12，yield274％Theeffectofsolventonsynthesiswasstudied。TheresultshowedthattheyieldwashigherinthepoorpolarsolventThesynthessofcampptotheein—Succi

9、nicAnhydridewasperformedinthemicrowaveconditionTheyieldwasthehighest，upto291％，in5hC、Thebi—esterofhydroxycamptothecinwasprepaedfromhydroxycamptothecinandsuccinicadhydridewith4dimethylaminopyridineasthecatalystat40℃yield82