One-Step Assembly of Carbamoyl-Substituted Heteroannelated [1,4]Thiazepines

We present a convenient synthesis of novel heteroaryl-fused 3-oxo-1,4-thiazepine-5-carboxamides and
5-oxo-1,4-thiazepine-3-carboxamides using a modification of four-component Ugi condensation. We
demonstrate the usefulness and versatility of the developed approach for the synthesis of variously
substituted compounds and discuss the scope and limitations of the chemistry involved.

我们报道了一种经改性的四组分Ugi缩合反应方法，可便捷合成新型杂芳环稠合的3-氧代-1,4-硫氮杂卓-5-甲酰胺与5-氧代-1,4-硫氮杂卓-3-甲酰胺类化合物。我们验证了所开发方法在合成各类取代化合物时的实用性与普适性，并对该反应体系的适用范围与局限性展开了讨论。