290832-40-5

Upstream product

• 614-96-0 5-methyl-1H-indole 
• 7394-79-8 3-(5-methyl-1H-indol-3-yl)propanoic acid 
• 5464-78-8 1-(2-methoxyphenyl)piperazine hydrochloride 

Downstream Products

• 290832-01-8 1-[4-(2-methoxy-phenyl)-piperazin-1-yl]-3-[5-methyl-2-(4-trifluoromethyl-phenyl)-1H-indol-3-yl]-propan-1-one 
• 290831-98-0 3-[2-(4-isopropyl-phenyl)-5-methyl-1H-indol-3-yl]-1-[4-(2-methoxy-phenyl)-piperazin-1-yl]-propan-1-one 
• 290831-92-4 1-{3-[2-(4-chlorophenyl)-5-methyl-1H-indol-3-yl]-1-oxopropyl}-4-(2-methoxyphenyl)piperazine 
• 290830-49-8 1-{3-[2-(4-bromophenyl)-5-methyl-1H-indol-3-yl]-1-oxopropyl}-4-(2-methoxyphenyl)piperazine 
• 290832-42-7 1-[3-(2-bromo-5-methyl-1H-indol-3-yl)-1-oxopropyl]-4-(2-methoxyphenyl )piperazine 

Relevant academic research and scientific papers

2-Aryl indole NK1 receptor antagonists: Optimisation of the 2-aryl ring and the indole nitrogen substituent

Novel 2-aryl indole hNK1 receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK1 receptor binding affinity and good brain penetration (e.g., 9d) were synthesised.

2-aryl indole derivative as antagonists of tachykinins

The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.

2-Aryl indole NK1 receptor antagonists: Optimisation of indole substitution

The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.