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1、第22卷第3期精细化工Vol.22,No.32005年3月FINECHEMICALSMar.2005医药与日化原料3右旋糖酐2阿司匹林偶联物的合成1,2111姚日生,高文霞,邓胜松,徐琪(1.合肥工业大学制药工程系,安徽合肥230009;2.合肥工业大学生物化工教育部重点实验室,安徽合肥230009)1摘要:以右旋糖酐和乙酰水杨酰氯为原料,合成了高分子偶联物右旋糖酐2阿司匹林,并用FTIR、HNMR对其结构进行了表征。考察了缚酸剂、右旋糖酐重均相对分子质量、反应温度和物料比对酯化反应的影响。结果表明,三乙
2、胺和吡啶均可作为该酯化反应的缚酸剂,而浓氢氧化钠水溶液则不适合;乙酰水杨酰基的接入率随右旋糖酐重均相对分子质量的增大而减小,但随乙酰水杨酰氯与右旋糖酐的质量比的增加而增大;当选用Mw=20000的右旋糖酐、缚酸剂三乙胺,反应温度在60℃左右、m(乙酰水杨酰氯)/m(右旋糖酐)=3106时,乙酰水杨酰基的接入率和其有效转化率分别为9130%和3107%。关键词:右旋糖酐2阿司匹林偶联物;右旋糖酐;阿司匹林中图分类号:TQ463文献标识码:A文章编号:1003-5214(2005)03-0205-04Synt
3、hesisofDextran2aspirinConjugate1,2111YAORi2sheng,GAOWen2xia,DENGSheng2song,XUQi(1.DepartmentofPharmaceuticalEngineering,HefeiUniversityofTechnology,Hefei230009,Anhui,China;2.KeyLaboratoryofBio2process,MinistryofEducation,HefeiUniversityofTechnology,Hefei2
4、30009,Anhui,China)Abstract:Inordertoobtainasustainedreleaseaspirinderivativehavinglessside2effectongastrointestinaltract,dextran2aspirinconjugatewaspreparedbycouplingreactionbetweeno21acetoxybenzoylchlorideanddextran.ItsstructurewascharacterizedwithFTIRan
5、dHNMR.Influencesofvariousfactors,suchasacidabsorbent,molecularweightofdextran,reactiontemperatureandmassratioofreactants,onthisreactionwereinvestigated.UVspectrumwasappliedtoevaluatethedrug2loadingratioofdextran2aspirinconjugateproducedunderdifferentreact
6、ionconditions.Theresultsshowthatbothtriethylamineandpyridineareeffectiveacidabsorbentsinthisreaction,whilesodiumhydroxidesolutioncouldnotbeusedasacidabsorbent.Thedrug2loadingratioofdextran2aspirinconjugatedecreaseswithincreaseinaveragemolecularweightofdex
7、tran,whileincreaseswithincreaseinmassratioofo2acetoxybenzoylchloridetodextran.Thus,reactionofo2acetoxybenzoylchlorideanddextranhavingaveragemolecularweightof20,000inmassratioof3106wascarriedoutat60℃,usingdimethylsulphoxideassolventandtriethylamineasacidab
8、sorbent.Undertheseoptimumreactionconditions,thedrug2loadingratioabout9130%andtheconvertingefficencyabout3107%wereattained.Keywords:dextran2aspirinconjugate;dextran;aspirin[3～5][6]阿司匹林是良好的解热、镇痛、抗炎药,20世纪后半期,力。但服用阿司匹林时
