190064-88-1

Upstream product

• 98-59-9 p-toluenesulfonyl chloride 
• 190064-87-0 3-ethyl-2-methyl-6-hydroxymethyl-4,5,6,7-tetrahydroindol-4-one 
• 190064-86-9 3-ethyl-2-methyl-6-acetoxymethyl-4,5,6,7-tetrahydroindol-4-one 
• 24941-58-0 3,5-dimethoxycyclohexa-2,5-diene-1-carboxylic acid 
• 90612-16-1 (3,5-dimethoxycyclohexa-2,5-dien-1-yl)methanol 
• 500583-06-2 3-ethyl-6-methoxymethyl-2-methyl-1,5,6,7-tetrahydro-indol-4-one 
• 500583-02-8 3-(2-hydroxy-1-methyl-butylamino)-5-methoxymethyl-cyclohex-2-enone 
• 32818-79-4 2-(hydroxyimino)pentan-3-one 
• 116836-16-9 2-amine-3-pentanol 

Relevant academic research and scientific papers

New cyclic butyrophenone derivatives in the indole series as potential atypical antipsychotics. A simple and practical synthesis of 6-aminomethyl-tetrahydroindol-4-ones and their affinities for D2 and 5-HT(2A) receptors

A simple and efficient synthesis of novel 6-aminomethyl-tetrahydroindol-4-ones, which are butyrophenone analogues of molindone, is described. These compounds exhibit potent affinities for D2 and 5-HT(2A) receptors in vitro. The most active compounds, 6d (QF 0408B) and 6e (QF 0409B), with pK(i) (5-HT(2A)/D2) ratios of 1.32 and 1.17 respectively, show an antipsychotic profile according to Meltzer's classification.

New synthetic approaches to CNS drugs. A straightforward, efficient synthesis of tetrahydroindol-4-ones and tetrahydroquinolin-5-ones via palladium-catalyzed oxidation of hydroxyenaminones

We have developed a facile and efficient synthesis of new conformationally restricted butyrophenones in the indole and quinoline series via palladium-catalyzed oxidation of hydroxyenaminones, and subsequent cyclization followed by spontaneous aromatizatio

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.