Abstract This contribution describes a novel Arndt–Eistert approach for the efficient synthesis of the potent and selective 5-HT7-antagonist,(R)-3-(2-(2-(4-methylpiperidin-1-yl)-ethyl) pyrrolidine-1-sulfonyl) phenol (SB-269970), from d-proline. The synthesis was carried out in 10 steps with an overall yield of 23%.
