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Updated: Jun 28, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
Amino- and hydroxy-functionalized 11-azaartemisinins and their derivatives
Ajit Shankar Singh1, Ved Prakash Verma, Mohammad Hassam
1Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow-226001, India.
Abstract:
An efficient conversion of artemisinin 1 into three new amino- and hydroxy-functionalized 11-aza prototypes 9, 11, and 12 has been achieved on a multigram scale by reaction with hydrazine, hydroxylamine, and 2-amino ethanol, respectively. Of these, 9 has been further diversified into a wide range of derivatives including imines, amines, amides, and linker based dimers. Prototypes 11 and 12 have been converted into the corresponding ethers in high yields. Some of these compounds have shown a high order of activity against multidrug-resistant malaria in mice by oral route.
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