反应详情

The procedure described for 5c was used. Deprotection of 5a and coupling with 121 mg of (2S)-2-[[(4-methoxy-2,3,6-trimethylphenyl)sulfonyl]amino]butanedioic acid 4-(1,1-dimethylethyl)ester (prepared from Asp(OtBu)-OH and (4-methoxy-2,3,6-trimethylphenyl)sulfonylchloride using the procedure described for 5b) yielded after purification 8 as a mixture of diastereomers (1:1). 1H-NMR 200 MHz (CD3OD) δ: 1.30 and 1.35 (9H, 2×s), 1.38-1.70 (6H, m), 2.12 and 2.14 (3H, 2×s) 2.18-2.51 (2H, m), 2.53 and 2.54, (3H, 2×s), 2.63 (3H, s), 2.85-3.54 (6H, m), 3.81 and 3.86 (3H, 2×s), 3.95-4.11 (1H, m), 5.03-5.21 (1H, m), 6.73 and 6.75 (1H, 2×s), 7.17-7.24 (1H, m), 7.52-7.78 (3H, m), 8.30-8.38 (1H, m).

1. customyielded
2. customafter purification 8
3. additionas a mixture of diastereomers (1:1)