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1、THEORGANICCHEMISTRYOFDRUGSYNTHESISVOLUME3DANIELLEDNICERAnalyticalBio-ChemistryLaboratories,Inc.Columbia,MissouriLESTERA.MITSCHERTheUniversityofKansasSchoolofPharmacyDepartmentofMedicinalChemistryLawrence,KansasAWILEY-INTERSCIENCEPUBLICATIONJOHNWILEYANDSONSNewYork?Chl
2、chester?Brisbane*Toronto?SingaporeCopyright?1984byJohnWiley&Sons,Inc.Allrightsreserved.PublishedsimultaneouslyinCanada.ReproductionortranslationofanypartofthisworkbeyondthatpermittedbySection107or108ofthe1976UnitedStatesCopyrightActwithoutthepermissionofthecopyrighto
3、wnerisunlawful.RequestsforpermissionorfurtherinformationshouldbeaddressedtothePermissionsDepartment,JohnWiley&Sons,Inc.LibraryofCongressCatalogingInPublicationData:(Revisedforvolume3)Lednicer,Daniel,1929-Theorganicchemistryofdrugsynthesis."AWiley-lntersciencepublicat
4、ion."Includesbibliographicalreferencesandindex.1.Chemistry,Pharmaceutical.2.Drugs.3.Chemistry,Organic—Synthesis.I.Mitscher,LesterA.,jointauthor.II.Title.[DNLM1.Chemistry,Organic.2.Chemistry,Pharmaceutical.3.Drugs—Chemicalsynthesis.QV744L473o1977]RS403.L38615M976-2838
5、7ISBN0-471-09250-9(v.3)PrintedintheUnitedStatesofAmerica10907654321Withgreatpleasurewededicatethisbook,too,toourwives,BeryleandBetty.ThegreattragedyofScienceistheslayingofabeautifulhypothesisbyanuglyfact.ThomasH.Huxley,"BiogenesisandAbiogenisis"PrefaceIhefirstvolumei
6、nthisseriesrepresentedthelaunchingofatrialballoononthepartoftheauthors.Inthefirstplace,wowerenotentirelyconvincedthatcontemporarymedicinal(hemistrycouldinfactbeorganizedcoherentlyonthebasisoforganicchemistry.If,however,onegrantedthatthismightbedone,wewerenotatallcert
7、ainthattheexercisewouldengageIheinterestofothers.Thatbook'sreceptionseemedtogivenriaffirmativeanswertoeachofthesequestions.Thesecondvolumewaspreparedlargelytofillgapsinthecoverageandtobringdevelopmentsinallfieldsuptoacommondate-1976.Intheprocessofpreparingthosevolume
8、s,weformedthehabitofscrutenizingtheliteraturefornewnonproprietarynamesasmiindicationofnewchemicalentitiesinorabouttobeinthe?linic.I