165963-38-2

Upstream product

• 110-91-8 morpholine 
• 144219-63-6 ethyl 1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylacetate 
• 98-09-9 benzenesulfonyl chloride 
• 165963-37-1 N-(3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylacetyl)morpholine 
• 165963-35-9 diethyl 1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolyl-malonate 
• 165963-34-8 1-benzenesulfonyl-5-bromo-3-ethyl-2-methyl-4,5,6,7-tetrahydroindol-4-one 
• 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 
• 6116-76-3 3-ethyl-2-methyl-4-oxo-1H-4,5,6,7-tetrahydroindole 
• 165963-36-0 3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolylmalonic acid 

Downstream Products

• 165963-40-6 N-<1β-(1-benzenesulfonyl-3-ethyl-2-methyl-4-oxo-4,5,6,7-tetrahydro-5-indolyl)ethyl>morpholine 
• 165963-39-3 N-<β-(1-benzenesulfonyl-3-ethyl-2-methyl-4-hydroxy-4,5,6,7-tetrahydro-5-indolyl)ethyl>morpholine 

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.