Asymmetric synthesis of a dopamine D1 agonist, dihydrexidine from D-serine

作者：Malhotra Rajesh; Ghosh Amit; Ghosh Rajib; Chakrabarti Sagar; Dutta Swarup; Dey Tushar K; Roy Subho; Basu Sourav^*; Hajra Saumen

来源：Tetrahedron: Asymmetry , 2011, 22(14-15): 1522-1529.

DOI：10.1016/j.tetasy.2011.08.014

A scalable asymmetric synthesis of trans-2-amino-6,7-dimethoxy-1-phenyltetralin 2 and its N-nosyl derivative 12 have been achieved from Garner aldehyde derived from easily available D-serine using a stereoselective PhMgBr addition, Wittig reaction and TFA-mediated Friedel-Crafts cyclization as the key steps. The synthesis of dihydrexidine is accomplished from the N-nosyl-2-amino-1-phenyltetralin 12.

• 出版日期2011-7-31