| 摘要 |
<p>A novel process for the preparation of α-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the α-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R4-X, wherein R4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The α-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of α-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H^_-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R4 is 1-(1-cycloalkenyl) are novel.</p> |
