919286-21-8Relevant articles and documents
Palladium Catalyzed C?O Coupling of Amino Alcohols for the Synthesis of Aryl Ethers
Mikus, Malte S.,Sanchez, Carina,Fridrich, Cary,Larrow, Jay F.
, p. 430 - 436 (2020)
Amine containing aryl ethers are common pharmacophore motifs that continue to emerge from drug discovery efforts. As amino alcohols are readily available building blocks, practical methodologies for incorporating them into more complex structures are highly desirable. We report our efforts to explore the application of Pd-catalyzed C?O coupling methods to the arylation of 1,2- and 1,3-amino alcohols. We established general and reliable conditions, under which we explored the scope and limitations of the transformation. The insights gained have been valuable in employing this methodology within a fast-moving drug discovery environment, which we anticipate will be of general interest to the synthesis and catalysis communities.
3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists: Part 1
Epple, Robert,Russo, Ross,Azimioara, Mihai,Cow, Christopher,Xie, Yongping,Wang, Xing,Wityak, John,Karanewsky, Don,Gerken, Andrea,Iskandar, Maya,Saez, Enrique,Martin Seidel,Tian, Shin-Shay
, p. 4376 - 4380 (2007/10/03)
We report the identification of a novel series of trisubstituted isoxazoles as PPAR activators from a high-throughput screen. A series of structural optimizations led to improved efficacy and excellent functional receptor selectivity for PPARδ. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif.
