Catalyst-Controlled Regiodivergent Dehydrogenative Heck Reaction of 4-Arylthiophene/Furan-3-Carboxylates
A catalyst-controlled regiodivergent dehydrogenative Heck reaction of 4-arylthiophene/furan-3-carboxylates has been realized. Use of a palladium catalyst led to the C-5 alkenylation through electronic palladation, while a ruthenium catalyst favored the C-2 alkenylation with the assistance of a directing group. This reaction exhibited good to excellent regioselectivities. (Figure presented.).
Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists
Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action in a rat model than tiotropium bromide.