Studies On Synthesis And Properties Of Novel Thiopyranothienopyrimidinone Derivatives

Thienopyrimidine derivatives have been found to show widespread biological activities,such as fungicide,herbicide,pesticide and medicine,and have extensively applied prospect.In this paper,we studied the synthesis of novel thienopyrimidine derivatives via aza-Wittig reaction which has been known for its available materials,mild condition and high yield.The conditions for cyclization were researched.The spectrum characteristics and biological activities of some compounds were also researched.And some of them were found to show good fungicidal activities.It can be summarized as follows:1.The novel carbodimide reacted with primary amines and second amines to give thiopyranothienopyrimidine derivatives via aza-Wittig reaction catalyzed by sodium alkoxide.Thirty novel compounds were synthesized.â… 2-alkylamino-thiopyranothieno[2,3-d]pyrimidin-4-ones(13)â…¡2-dialkylamino- thiopyranothieno[2,3-d]pyrimidin-4-ones(17)2.The carbodimide reacted with,alcohols or phenols to give thiopyranothienopyrimidine derivatives via aza-Wittig reaction catalyzed by sodium alkoxide or potassium carbonate.Eleven novel compounds were synthesized.â…¢2-alkyl(aryl)oxyl-thiopyranothieno[2,3-d]pyrimidin-4-ones(11)3.The cyclization of carbodiimide with amines and alcohols was in presence of sodium alkoxide.But the cyclization of earbodiimide with phenols was in solid potassium carbonate.The selectivity of cyclization related to both steric hindrance and election of primary amine.