Abstract

Urease, a nickel-dependent enzyme, has a powerful catalytic activity to decompose urea into ammonia via hydrolysis reaction under mild condition. In the present work, urease was employed for the synthesis of two series of polyhydroquinoline and polyhydroacridine derivatives via one-pot condensation of the ammonia generated in situ from urea, aryl aldehydes, and dimedone or ethyl acetoacetate (i.e., Hantzsch-type reaction) in water under mild green condition. The valuable features of this enzymatic method are mild reaction conditions, short reaction times, wide substrate toleration, and high yield of products. The present work provides a novel enzymatic catalysis to synthesize polyhydroquinolines and polyhydroacridines and expands the application of urease in organic synthesis.

Graphic abstract

中文翻译：

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脲酶：一种高效生物催化剂，用于从原位形成的氨合成聚氢喹啉和聚氢吖啶。

 抽象的

脲酶是一种镍依赖性酶，具有强大的催化活性，可在温和条件下通过水解反应将尿素分解为氨。在本工作中，脲酶用于通过尿素、芳基醛和双甲酮或乙酰乙酸乙酯原位产生的氨的一锅缩合（即Hantzsch型反应）合成了两个系列的聚氢喹啉和聚氢吖啶衍生物。水在温和的绿色条件下。该酶法的显着特点是反应条件温和、反应时间短、底物耐受性广、产物收率高。本工作提供了一种新型酶催化合成聚氢喹啉和聚氢吖啶的方法，拓展了脲酶在有机合成中的应用。

 图文摘要