TMSCl Promated Reaction Of Organozinc Reagents Nitrones And Preparation Of Pyrimidines Thiourean And Determination Of Their Bioactivities

Organozinc reagent is one of the earliest prepared organometallics in organic synthesis. Organozinc reagents have already represented many advantages, such as excellent functionality compatibility, high chemoselectivity, regioselectivity and stereoselectivity etc. in organic synthetic chemistry because of their low reactivity. Additionally, they also can undergo transmetalation with a variety of transition metal salts or complex leading to new transition metal compounds and the resulting organometallics can react with many organic electrophiles.Acylthiourea derivatives have been widely researched because of their broad in insecticidal, anti-fungal, anti-virus, herbicide and plant growth regulating properties during the past two or three decades. Acylthiourea derivatives contain oxygen, nitrogen and sulfur heteroatom compounds, besides a wide range of their bioactivities, they are important intermediates for the synthesis of many heterocyclic compounds.This thesis includes four chapters.Chapter one:The development of preparation and reaction of organozinc reagentsThe preparation organozinc reagents and their application in organic synthesis were reviewed in detail.Chapter two:TMSCl promoted reaction of organozinc reagents with nitronesIn the presence of Lewis acid (TMSCl), reaction of organozinc reagents with nitrone give hydroxylamine compounds which were further reduced to corresponding amines.Chapter three:The development of acylthiourea compoundsResearch on the synthesis and applications of thioureas was briefly reviewed.Chapter four:Research on the synthesis and biological activity of pyrimidine thiourea.Pyrimidinyl and triazolopyrimidinyl amines reacted with acylisothiocyanates to give corresponding pyrimidine thiourea compounds. The preliminary biologic tests showed that 4 of these compounds had good activity as plant growth regulators.