Novel pathway for the synthesis of arylpropionamide-derived selective androgen receptor modulator (SARM) metabolites of andarine and ostarine

作者：Schragl Katharina M; Forsdahl Guro; Gmeiner Guenter; Enev Valentin S^*; Gaertner Peter

来源：Tetrahedron Letters, 2013, 54(18): 2239-2242.

DOI：10.1016/j.tetlet.2013.02.065

• Selective androgen receptor modulators
• Andarine/ostarine metabolites
• Arylpropionamides
• Amide bond formation

O-Dephenylandarine and O-dephenylostarine, two SARM metabolites relevant for doping control analysis, were synthesized in their endogenous (S)-forms as well as in terms of their racemates. The enantiopure (S)-metabolites were obtained after six steps in 20% and 23% overall yield, the slightly modified racemic route provided the compounds in 28% and 31% total yield, respectively.

• 出版日期2013-5-1