Paper
1,3-Dibromo-1,1-difluoro-2-propanone as a Useful Synthon for a Chemoselective Preparation of 4-Bromodifluoromethyl Thiazoles
Published Nov 5, 2018 · Marco Colella, P. Musci, C. Carlucci
ACS Omega
Q2 SJR score
6
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0
Influential Citations
Abstract
We report herein a synthetic protocol for the preparation of 1,3-dibromo-1,1-difluoro-2-propanone, a new synthon used for the first time in a reaction with aromatic amines and sodium thiocyanate, leading to thiazoles which are useful candidates in drug discovery programs. The new synthon allows to introduce a bromodifluoromethyl group at the C4 of the thiazole, and it is amenable of further transformation such as the Br/F exchange useful in radiopharmaceutics. Application of the strategy to the preparation of a precursor of the biologically relevant DF2755Y is also reported.
Study Snapshot
This study presents a new synthetic protocol for preparing 1,3-dibromo-1,1-difluoro-2-propanone, a useful synthon for drug discovery programs, leading to 4-bromodifluoromethyl thiazoles.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
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