Publications by authors named "Megan E Neubig"
Article Synopsis
- Researchers discovered a strong and selective antagonist for the lysophosphatidic acid receptor 1 (LPAR1), which has antifibrotic properties, initially validated through a specific assay involving MRTF-A.* -
- Structural modifications improved the compound's stability and pharmacokinetics, leading to a promising candidate for oral dosing that effectively blocked LPA-induced histamine release and showed efficacy against lung fibrosis in preclinical tests.* -
- Despite its potential, the development of the LPAR1 antagonist was discontinued due to observed CNS toxicity in dog models, raising safety concerns for clinical use in idiopathic pulmonary fibrosis (IPF).*
The biological properties of trifluoromethyl compounds have led to their ubiquity in pharmaceuticals, yet their chemical properties have made their preparation a substantial challenge, necessitating innovative chemical solutions. We report the serendipitous discovery of a borane-catalyzed formal C(sp)-CF reductive elimination from Au(III) that accesses these compounds by a distinct mechanism proceeding via fluoride abstraction, migratory insertion, and C-F reductive elimination to achieve a net C-C bond construction. The parent bis(trifluoromethyl)Au(III) complexes tolerate a surprising breadth of synthetic protocols, enabling the synthesis of complex organic derivatives without cleavage of the Au-C bond.
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