College of Chemistry and Chemical Engineering , Jiangxi Normal University , Nanchang 330022 , China.
J Org Chem. 2018 Mar 16;83(6):3403-3408. doi: 10.1021/acs.joc.8b00068. Epub 2018 Mar 7.
The synthesis of N-acyl-5-halo-8-aminoquinolines has been realized by directly employing 8-aminoquinolines and acyl halides (Cl, Br, I) with copper catalysis. The construction of the target products involves domino N-acylation and C5-H halogenations of the 8-aminoquinoline, wherein the acyl halides act as the donors of both acyl and halide atoms, which enables the first access to the step efficient synthesis of 5-halogenated N-acyl quinlolines.
N-酰基-5-卤代-8-氨基喹啉的合成立即在铜催化下直接利用 8-氨基喹啉和酰卤（Cl、Br、I）实现。目标产物的构建涉及 8-氨基喹啉的串联 N-酰化和 C5-H 卤化，其中酰卤作为酰基和卤原子的供体，这使得首次实现了 5-卤代 N-酰基喹啉的高效合成。
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