[EN] NITROGEN-CONTAINING HETEROARYL DERIVATIVES<br/>[FR] DÉRIVÉS HÉTÉROARYLIQUES CONTENANT DE L'AZOTE
申请人:HOFFMANN LA ROCHE
公开号:WO2011089132A1
公开(公告)日:2011-07-28
The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
A highly regioselective reaction of<i>N</i>-fluoropyridinium salts with stabilized sulfur, oxygen, and nitrogen nucleophiles: A convenient route to 2-substituted pyridines
作者:Alexander S. Kiselyov、Lucjan Strekowski
DOI:10.1002/jhet.5570300530
日期:1993.10
2-Substitutedpyridines are efficiently obtained by the reactions of N-fluoropyridinium tetrafluoroborate or triflate with anions derived from benzenethiols, phenols, azoles, cyanamide, and with azide anion. The results are consistent with a nucleophile addition at the position 2 of the N-fluoropyridinium cation as the major reaction pathway.
The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I)
wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.