由N-酰基-a-氨基酸合成5(4H)-噁唑酮的新方法

A New Method foir the Synthesis of 5(4H)-Oxazolones from N-Acyl-a-Amiho Acids

在碳酸钾、丙酮的水溶液中由N-酰基四氢噻唑-2-硫酮进行氨基酸解得到10种N-酰基-α-氨基酸Ⅰ_a-(?)发现在三聚氯氰及三乙胺存在下,由N-酰基-α-氨基酸环合成8种饱和5(4H)-(口恶)唑酮Ⅱ_a-h的新方法,进而在硫酸铁催化下得到10种不饱和5(4H)-(口恶)唑酮衍生物Ⅲ_a-(?)

In K2CO3-CH3COCH3-H2O system, N-acyl-a-amino acids ( Ⅰ a-j) were prepared by the reaction of amino acids with N-acyl thiazolidines-2-thiones and the yields were 76%-95%. The synthesis of saturated 5(4H)-oxazolones( Ⅱa-h) from I under mild reaction conditions in yields of 43% - 84% by the use of cyanuric chloride as a condensing reagent in the presence of triethylamine was reported. Unsaturated 5(4H)-oxazolones (Ⅲa-1) were obtained from I in the yields of 43%-93% by the aldol reaction in which Fe2SO4)3 was used as a catalyst.