由N-酰基-a-氨基酸合成5(4H)-噁唑酮的新方法

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-j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)-噁唑酮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)-噁唑酮衍生物Ⅲ_a-j

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

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(Ⅱ_a-h) from Iunder 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 (Ⅲ_a-j) were obtained from Iin the yields of 43%～93% by the aldol reaction in which Fe₂SO₄)₃ was used as a catalyst.