685126-90-3Relevant articles and documents
Multigram Synthesis of Tetrasubsituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow
Alder, Catherine M.,Gray, Matthew,Huff, Chelsea A.,Manning, Calvin O.,Preston, Alex,Rushworth, Philip,Shuster, Leanna E.,Watson, Robert J.,Wheelhouse, Katherine M. P.,Williams, Glynn D.,Demont, Emmanuel H.
, p. 365 - 379 (2022/02/10)
This article describes two routes toward the synthesis of cis or trans C2,3,5,7-tetrasubstituted dihydrobenzofurans as potent and selective bromodomain and extra-terminal BD2 inhibitors, followed by the optimization of the synthesis of the lead molecule GSK973 to support pre-clinical efficacy and safety studies. The use of flow chemistry for a Claisen rearrangement, extensive optimization of the fluorination step, and high-yielding aminocarbonylation were key to generate the required 50 g of material. The identified new route also represents a robust starting point for further optimization.
Melanocortin-4 receptor binding compounds and methods of use thereof
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Page 92, (2008/06/13)
Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are a
