45 research outputs found
Highly Regioselective Protecting-Group-Free Synthesis of the Antimalarial Drug MMV693183
MMV693183 is a promising
antimalarial drug candidate that works
for uncomplicated malaria treatment and resistance management. Herein,
we report an efficient and highly regioselective synthesis of MMV693183.
This novel synthetic method highlights a three-step route with an
overall yield of 46% from readily available starting materials. The
key to the success lies in (1) utilizing the subtle difference of
the two amino groups in the starting material (S)-propane-1,2-diamine
dihydrochloride without amino protection and (2) identifying the L-(+)-tartaric acid as the counter acid for the organic
salt formation, yielding the desired regioisomer up to 100:0. The
efficient and scalable three-step protocol operates under mild conditions
with a high chemo/regioselectivity, providing effective access to
MMV693183