<jats:title>Abstract</jats:title><jats:p>Three new guaipyridine sesquiterpene alkaloids, rupestine A, B, C (<jats:bold>1</jats:bold>–<jats:bold>3</jats:bold>, resp.), and the new nor‐sesquiterpne alkaloid rupestine D (<jats:bold>4</jats:bold>) were obtained from the flowers of <jats:italic>Artemisia rupestris</jats:italic> L. Their structures were elucidated on the basis of sepectroscopic data and by comparison with those of the related compounds reported in the literature. In addition, the absolute configurations of <jats:bold>2</jats:bold> and <jats:bold>4</jats:bold> were determined by single‐crystal X‐ray diffraction analyses.