Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 11, Issue 3, Pages 341-345Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op060244p
Keywords
-
Categories
Ask authors/readers for more resources
The manufacturing process for lumefantrine, 2, one of the two active principles in the fixed-dose combination of the antimalarial drug Coartem, was reworked. For the conversion of 2-chloro-1-(2,7-dichloro-9H-fluoren-4-yl)ethanone, 5, to 2-dibutylamino-1-(2,7-dichloro-9H-fluoren-4-yl)ethanol, 8, a one-pot process was developed that eliminated isolation of the epoxide 2-(2,7-dichloro-9H-fluoren-4-yl)oxirane, 7. Significant increase in throughput was achieved by applying new reaction and crystallization conditions for the Knoevenagel condensation of 2-dibutylamino-1-(2,7-dichloro-9H-fluoren-4-yl)ethanol, 8, to 2-dibutylamino-1-{2,7-dichloro-9-[1-(4-chlorophenyl)meth-(Z)-ylidene]-9H-fluoren-4-yl}ethanol, 2.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available