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N-酰基-2-硫酮氢化噻唑在合成酯、酰胺、醛、二醇等,特别是在不对称的Aldol反应中得到了应用。用三聚氯氰在三乙胺存在下,使羧酸与2-硫酮氢化噻唑反应,直接分子间脱水缩合,成功地得到了N-酰基-2-硫酮氢化噻唑。本文报道了另一种新的合成方法,在三乙胺存在下,由饱和5(4H)-噁唑酮与2-硫酮氢化噻唑反应合成了N-酰基-2-硫酮氢化噻唑(I),并由此进一步得到了N-酰基二肽和三肽(Ⅱ_(a～d))。
N-acyl-2-thione Hydrogenated thiazoles are used in the synthesis of esters, amides, aldehydes, glycols and the like, especially in asymmetric Aldol reactions. With cyanuric chloride in the presence of triethylamine, the carboxylic acid is reacted with 2-thione hydrogen thiazole, and the direct dehydration condensation between molecules has succeeded in obtaining N-acyl-2-thione hydrogen thiazole. In this paper, we report another new synthetic method for the synthesis of N-acyl-2-thione hydrazinothiazoles by the reaction of saturated 5 (4H) -oxazolone with 2-thione hydrazide in the presence of triethylamine ), And further N-acyl dipeptide and tripeptide (II_ (a ~ d)) were obtained.