Site-selective C5-H and <i>N</i>-H alkylation of unprotected 8-aminoquinolines

8-Aminoquinolines are the building blocks of many pharmaceutical compounds, which has motivated the scientific community to develop new ways to derivatize these compounds. In this work, we performed a site-selective C5-H and N-H alkylation of 8-aminoquinolines using para-quinone methides under extremely mild conditions. C5-H alkylation was performed using protecting group-free 8-aminoquinolines and in metal-free conditions. N-H alkylations were also carried out under mild conditions. All corresponding alkylation products were obtained in high to excellent yields.

Journal

CHEMICAL COMMUNICATIONS

Year

2022

Volume

58

Issue

31

Pages

4893-4896

ISSN

1359-7345

eISSN

1364-548X

DOI

10.1039/d2cc00780k

WoS UID

WOS:000775185200001

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