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A Coupling-Isomerization Sequence As An Entry To A Novel Three Component One-Pot Synthesis of 1,5-Benzoheteroazepines
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1  Department Chemie, Ludwig-Maximilians-Universitat München, Butenandtstr. 5-13 (Haus F), D-81377 München, Germany

Abstract: 2,4-Di(hetero)aryl substituted 2,3-dihydro 1,5-benzodiazepines, -oxazepines, and thiazepines can be readily synthesized in a three component one-pot process initiated by a coupling-isomerization sequence of an electron poor (hetero)aryl halide and a terminal propargyl alcohol subsequently followed by a cyclocondensation with 2-amino, 2-hydroxy, or 2-mercapto anilines.
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