Abstract A facile and conveniently simple new protocol is devised for the synthesis of 3,5-disubstituted and annulated isothiozoles under transition metal and catalyst free conditions utilizing easily available acetophenones, dithioesters and NH4OAc. This strategy involves C=O and C=S functionalization via sequential imine formation followed by intra molecular cyclization and aerial oxidation forming consecutive C−N and S−N bonds respectively in one pot. This protocol offers a low cost, user friendly, straight forward and widely applicable approach to 3,5-disubstituted isothiazoles. Graphical Abstract

中文翻译：

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在无金属条件下使用苯乙酮和二硫酯合成 3,5-二取代异硫唑的新方法

摘要 为了在过渡金属和无催化剂条件下利用容易获得的苯乙酮、二硫酯和 NH4OAc 合成 3,5-二取代和环状异硫唑，设计了一种简便易行的新方案。该策略涉及通过依次形成亚胺，随后分子内环化和空气氧化在一个锅中分别形成连续的 C-N 和 S-N 键的 C=O 和 C=S 功能化。该协议为 3,5-二取代异噻唑提供了一种低成本、用户友好、直接且广泛适用的方法。图形概要