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1、Pictet–Spengler反应论文：β-咔啉类生物碱的合成及其生物活性【中文摘要】β-咔啉类生物碱,是吲哚类生物碱中非常重要的一类,它是由吲哚并吡啶构成的三环体系,结构简单,数量众多。主要分布于植物、海洋生物、蓝藻、蘑菇、动物（如非洲蛙）,甚至人体的组织、血液中。这类生物碱种类繁多,生物活性广泛,如抗肿瘤活性、杀虫活性、抑菌活性、抗氧化活性、抗病毒活性、抗抑郁活性等等。本文主要根据β-咔啉生物碱在人体的代谢途径,分为两条路线来进行目标产物合成。主要的研究结果如下:1.路线一,以吲哚-3-甲醛为原料,通过Henry反应（超声波辅助）、LiAlH4【英文摘要】β-Carboli
2、neanditsderivativesshowgreatsignificancetoourlife,becauseoftheirimportanceinnaturalproductandbroadbioactiveactivitiessuchasantitumor,bacteriostasis,anti-oxidation,antiviral,antidepressantandsoon.Inthispaper,weusedthreecompoundsasstartingmaterialbytworoutes,thengot20compounds.thecompoundswere
3、identifiedandevaluatedonanti-bacterialactivity,insecticidalactivityandantitumoractivity.Theresultswerejustasfollows.(1).Route1,withIndoles-3–formaldehydeasstartingmaterial,throughHenryreactionfollowedbydeoxidationofLiAlH4,wegottryptamine,whichwasreactedwithmethanalandaldehyde,leadingtotetrah
4、ydro-β-Carbolines.thenthroughadehydrogenation,compoundsa-1anda-2weregotten.(2).Route1,wegotcompoundsa-13,a-14,a-15,a-16,a-17anda-20throughPictet–Spenglerreactionwith5-Methoxytryptaminereactedwithmethanal,aldehyde,propionaldehyde,butanal,isobutanal,benzaldehyde.(3).Route2,aPictet–Spenglerreac
5、tionbetweentryptophanandMethanal,aldehyde,propionaldehyde,butanal,isobutanal,benzaldehyde,m-nitrobenzaldehyde,o-nitrobenzaldehyde,anisaldehyde,3-methoxy-4-hydroxybenzaldehyde,o-hydroxybenzaldehyde,acetone,cyclohexanone,thenthroughadehydrogenation,wegotcompoundsa-1—a-12,a-18anda-19.(4).Allthe
6、compounds’Structureswereelucidatedmainlybasedon1~HNMR,(13)~CNMR,DEPTandESI-MS.Inthosecompounds,thereare7compounds(a-5、a-10、a-11、a-15、a-16、a-17anda-19)werenew.(5).Anti-bacterialactivityinvitroagainststaphylococcusaureus,Bacilluscereus,Bacillussubtilis,PseudomonasaeruginosaandEscherichiacoliof
7、compoundsa-1—a-12、a-18anda-19bytabletdiffusionmethod.Ithasbeenobservedthatcompoundsa-1,a-2,a-3anda-5showedexcellentactivity.(6).Insecticidalactivityagaistarmywormofallthecompoundsbyleafdiscmethod.Ithasbeenobservedthatallthecompoundsshownoobviousins
