| Literature DB >> 10882001 |
I Andreu1, D Cortes, P Protais, B K Cassels, A Chagraoui, N Cabedo.
Abstract
The preparation of N-methyl-BTHIQ (4) from N-phenylethyl-phenacetamide (1) by cyclization, reduction and N-alkylation in acid medium has been achieved in good yield in a 'one-pot' procedure. Acylation of imine (2) intermediate afforded the Z and E stereoselectivity in the enamide formation. 6-Hydroxy-BTHIQ (7) shows selectivity for D2 dopamine receptors, while its N-methylated homologue (8) displays higher affinities for both D1 and D2 receptor types, with an unexpected increase in D1 dopamine receptor affinity.Entities:
Mesh：
Substances：
Year: 2000 PMID： 10882001 DOI： 10.1016/s0968-0896(00)00027-4
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641