Synthesis Of Acylthioureas Derived From Acetylsalicylic Acid And Benorilate By Triphosgene

Chapter 1: The nature and the research progress of triphosgene.A brief review for the physical properties and existing synthetic methods and themain chemical properties of triphosgene.Chapter2: Synthesis by triphosgene and test of biological activities of N-aryl-N'-(2- acetyloxybenzoyl) Thioureas derivatives.The frist part: A brief review for the properties and use and existing syntheticmethods of acylthiourea.The second part:Using triphosgene as chloridizing reagent, a series of new Naryl-N'-(2- acetyloxybenzoyl)thioureas derivatives were synthesized by one-pot andphase-transfer catalytic method .Compared with the traditional method,This methodhas the advantages of green material and easy operation and high yield.Their structures are confirmed by FT-IR, 1H NMR ,13C NMR spectra and elementalanalysis. The preliminary biological activity tests show that some of the titlecompounds have good regulating activities for the growth of rape.Chapter 3: Synthesis by triphosgene and test of biological activities of 1-aryloxyacetyl-4-(2- acetyloxybenzoyl)thiosemicarbazide derivatives.A series of new 1-aryloxyacetyl-4-(2-acetyloxybenzoyl)thiosemicarbazidederivatives were synthesized green and high efficiently by serial reactions oftriphosgene, acetylsalicylic acid, ammonium thiocanate and aromatic amines, andconfirmed by FT-IR, ¹H NMR, ¹³C NMR spectra and elemental analysis.Thepreliminary biological activity tests show that some of the title compounds have someregulating activities for the growth of rape.Chapter 4: Synthesis of benorilate by triphosgene.The benorilate was synthesized by exploration of the best reative conditionssuch as univariate analysis, repeated test, using triphosgene as chlorinating agents. Thepurity of product were determined by the gas chromatography. Using triphosgene aschloridizing reagent, it has the advantages of milder reaction conditions,lesspollution,less by-product and safety. The water solution of PEG-6000 is used as catalyst, the reaction is carried through at room temperature,the yield of benorilatebecome greaterly higher.