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Title: Synthesis of Deuterated Endochin‐Like Quinolones
ABSTRACT

Malaria continues to be a serious and debilitating disease. The emergence and spread of high‐level resistance to multiple antimalarial drugs byPlasmodium falciparumhas brought about an urgent need for new treatments that will be active against multidrug resistant malaria infections. One such treatment,ELQ‐331(MMV‐167), an alkoxy carbonate prodrug of 4(1H)‐quinoloneELQ‐300, is currently in preclinical development with the Medicines for Malaria Venture. Clinical development ofELQ‐331or similar compounds will require the availability of isotopically labeled analogs. Unfortunately, a suitable method for the deuteration of these important compounds was not found in the literature. Here, we describe a facile and scalable method for the deuteration of 4(1H)‐quinoloneELQ‐300, its alkoxycarbonate prodrugELQ‐331, and their respective N‐oxides using deuterated acetic acid.

 
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PAR ID:
10506123
Author(s) / Creator(s):
 ;  ;  ;  ;  ;  ;  ;  
Publisher / Repository:
Wiley Blackwell (John Wiley & Sons)
Date Published:
Journal Name:
Journal of Labelled Compounds and Radiopharmaceuticals
Volume:
67
Issue:
5
ISSN:
0362-4803
Format(s):
Medium: X Size: p. 186-196
Size(s):
p. 186-196
Sponsoring Org:
National Science Foundation
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