Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist.
The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT2A antagonist 19.
Smith
A L
AL
Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Harlow, Essex, UK. adrian_smith@merck.com
Stevenson
G I
GI
Lewis
S
S
Patel
S
S
Castro
J L
JL
D001667:Binding, Competitive; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D014363:Tryptamines / Q000737:chemistry / Q000494:pharmacology
D007211:Indoles; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines