Adrian Leonard Smith

2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor

A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD2 receptors can be controlled by suitable C-2 aryl groups.

Traceless solid phase synthesis of 2,3-disubstituted indoles

Abstract An efficient method for the traceless solid phase synthesis of 2,3-disubstituted indoles using a THP linker and a Pd(0)-mediated annulation of 2-iodoaniline and acetylenes is reported.

An Efficient Solid‐Phase Synthetic Route to 1,3‐Disubstituted 2,4(1H,3H)‐Quinazolinediones Suitable for Combinatorial Synthesis

Abstract Novel, efficient solid phase chemistry has been developed for the synthesis of 1,3-disubstituted quinazolinediones. Anthranilic acids are linked to a chloroformate resin through the nitrogen, amines are coupled to the free carboxylic acid, and thermal cyclization leads to heterocycle formation and concommitant resin release resulting in traceless linkage.

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.