892405-35-5

Upstream product

• 892403-84-8 3-(3-methylaminomethylphenoxy)propan-1-ol 
• 42445-46-5 2-bromo-1-(4-methylsulfanyl-phenyl)-ethanone 
• 100-83-4 meta-hydroxybenzaldehyde 
• 245510-06-9 3-(3-hydroxy-propoxy)-benzaldehyde 

Downstream Products

• 892405-37-7 3-[2-methyl-4-(4-methylsulfanylphenyl)-1,2,3,4-tetrahydroisoquinolin-7-yloxy]propan-1-ol 
• 892405-39-9 methanesulfonic acid 3-[2-methyl-4-(4-methylsulfanyl-phenyl)-1,2,3,4-tetrahydro-isoquinolin-7-yloxy]-propyl ester 
• 892407-39-5 2-methyl-4-(4-methylsulfanyl-phenyl)-7-(3-morpholin-4-yl-propoxy)-1,2,3,4-tetrahydro-isoquinoline 
• 892405-33-3 7-[3-(4-fluoro-piperidin-1-yl)propoxy]-2-methyl-4-(4-methylsulfanylphenyl)-1,2,3,4-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors

A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H3 ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.

A practical synthesis of enantiopure 7-alkoxy-4-aryl- tetrahydroisoquinoline, a dual serotonin reuptake inhibitor/histamine H 3 antagonist

An efficient synthesis of compound 1 featuring a novel sequential Friedel-Crafts alkylation strategy to construct the 4-aryl- tetrahydroisoquinoline core structure has been developed. Resolution with (D/L)-di-p-toluoyl-tartaric acid is utilized to provide the enantiomerically pure material. Overall, the route is concise and amenable for large-scale synthesis.

TETRAHYDROISOQUINOLINE COMPOUNDS FOR TREATMENT OF CNS DISORDERS

Certain tetrahydroisoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor-and serotonin-mediated diseases.