反应详情

A solution containing 5-allyl-piperazine-1,3-dicarboxylic acid 1-benzyl ester 3-methyl ester, 3, (1.64 g, 5.1 mmol), N-Boc-allylglycine (3.9 g, 18.0 mmol) and 2-isobutoxy-1-isobutoxycarbonyl-1,2-dihydroquinoline (IIDQ) (5.5 g, 18.0 mmol) in THF was stirred at rt for 48 h. The solvent is removed in vacuo and the residue is purified over silica gel (EtOAc/hexane) to afford 1.28 g (48%) of 4. 1H NMR (CDCl3) δ 7.39 (m, 5H), 5.78 (m, 2H), 5.38–5.10 (m, 6H), 5.0–4.1 (series of m, 5H), 3.73 (br s, 3H), 2.66–2.20 (series of m, 7H), 1.45 (br s, 9H); MS 516 (M+H)+.

1. customThe solvent is removed in vacuo
2. customthe residue is purified over silica gel (EtOAc/hexane)