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2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES HAVING ANTIPSYCHOTIC ACTIVITY,AND SYNTHESIS OF ALPHA-SUBSTITUTED-ARYLACETAMIDES
2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES HAVING ANTIPSYCHOTIC ACTIVITY,AND SYNTHESIS OF ALPHA-SUBSTITUTED-ARYLACETAMIDES
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机译:具有抗菌活性的2,3,4,5-四氢-1H-3-苯并二氮杂并合成α-取代的芳酰胺
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PCT No. PCT/US93/01425 Sec. 371 Date Aug. 19, 1994 Sec. 102(e) Date Aug. 19, 1994 PCT Filed Feb. 23, 1993 PCT Pub. No. WO93/16997 PCT Pub. Date Sep. 2, 1993.A novel process for the preparation of alpha -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 alpha -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 alpha -substituted arylacetamides are useful as intermediates in the preparation (by reduction) of alpha -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.
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