235425-86-2

Upstream product

• 6116-76-3 3-ethyl-2-methyl-4-oxo-1H-4,5,6,7-tetrahydroindole 
• 98-09-9 benzenesulfonyl chloride 
• 235425-82-8 N¹-(1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylacetyl)-N⁴-(tert-butoxycarbonyl)piperazine 
• 165963-36-0 3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylmalonic acid 
• 165963-34-8 1-benzenesulfonyl-5-bromo-3-ethyl-2-methyl-4,5,6,7-tetrahydroindol-4-one 
• 144219-63-6 ethyl 1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylacetate 
• 144219-62-5 1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-1H-4,5,6,7-tetrahydroindole 
• 144219-66-9 3-ethyl-2-methyl-4-oxo-1H-4,5,6,7-tetrahydro-5-indoleacetic acid 
• 235425-84-0 N-(1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylacetyl)piperazine 
• 165963-35-9 diethyl 1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolyl-malonate 
• 235425-80-6 N-(tert-butyloxycarbonyl)-N'-(3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylacetyl)piperazine 

Downstream Products

• 235425-92-0 N-<β-(1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolyl)ethyl>piperazine 

Relevant academic research and scientific papers

Conformationally restricted butyrophenones with mixed dopaminergic (D2) and serotoninergic (5-HT(2A)) affinities. Synthesis of 5-aminoethyl-and 6- aminomethyl-4-oxotetrahydroindoles as potential atypical antipsychotics

We describe the synthesis of 5-aminoethyl- and 6-aminomethyl-4- oxotetrahydroindoles as butyrophenone derivatives in the indole series, as potential atypical antipsychotics. The affinities of these compounds for serotonin (5-HT(2A)) and dopamine (D2) receptors were evaluated in vitro. The ratios of pK(i)'s for 5-HT(2A)/D2 receptors may be useful for rapid screening of new compounds and assessing potential induction of extrapyramidal symptoms; ratio values ≥1.12 (Meltzer's ratio) are predictive of an atypical antipsychotic profile. Compounds 26e (QF 0408B) and 26f (QF 0409B) showed high affinity for both D2 and 5-HT(2A) receptors, and their Meltzer's ratios were 1.32 and 1.17 respectively, while haloperidol showed a ratio of 0.93.