Triethylamine → Ethyl 3-[4-(N-BOC-4-hydroxypiperidin-4-yl)phenyl]crotonate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A mixture of 10-3 (500 mg, 1.4 mmoles), ethyl crotonate (1.7 mL, 3.8 mmoles), Pd(OAc)2 (31 mg, 0.14 mmoles), NEt3 (0.78 mL, 8 mmoles), tri-o-tolylphosphine (170 mg, 0.56 mmoles), and CH3CN (7 mL) was heated in a sealed tube at 100° C. for 24 hours. The cooled reaction mixture was diluted with EtOAc and then washed with H2O, 10% KHSO4, saturated NaHCO3, and brine, dried (MgSO4), and concentrated. Flash chromatography (silica, 25% EtOAc/hexanes) gave 12-1 as a waxy yellow solid. Rf 0.33 (silica, 25% EtOAc/hexanes).

Herkunft & Nachweise