2,5-Dichlorothiophene-3-sulfonyl chloride → (r)-2,5-Dichloro-thiophene-3-sulfonic acid [1-(5'-fluoro-2'-methoxy-biphenyl-4-yl)-ethyl]-amide
反応式
[F:1][C:2]1[CH:3]=[CH:4][C:5]([O:27][CH3:28])=[C:6]([C:8]2[CH:13]=[CH:12][C:11]([C@H:14]([NH:16]S(C3C=C(C)OC=3C)(=O)=O)[CH3:15])=[CH:10][CH:9]=2)[CH:7]=1.[Cl:29][C:30]1[S:31][C:32]([Cl:39])=[CH:33][C:34]=1[S:35](Cl)(=[O:37])=[O:36].FC1C=CC(OC)=C(C2C=CC(C(N)C)=CC=2)C=1>>[F:1][C:2]1[CH:3]=[CH:4][C:5]([O:27][CH3:28])=[C:6]([C:8]2[CH:13]=[CH:12][C:11]([C@H:14]([NH:16][S:35]([C:34]3[CH:33]=[C:32]([Cl:39])[S:31][C:30]=3[Cl:29])(=[O:37])=[O:36])[CH3:15])=[CH:10][CH:9]=2)[CH:7]=1参加物
4
反応物 3
生成物 1
実験手順
Prepared in a similar manner to (R)-2,5-dimethyl-furan-3-sulfonic acid [1-(5′-fluoro-2′-methoxy-biphenyl-4-yl)-ethyl]-amide (Example 10) starting with 2,5-dichloro-3-thiophenesulfonyl chloride and 1-(5′-fluoro-2′-methoxy-biphenyl-4-yl)-ethylamine. Title compound: 1H NMR (400 MHz, CDCl3): δ 7.40, 7.18 (a/b, 4H), 7.05-6.88 (m, 4H), 5.05 (d, 1H), 4.60 (m, 1H), 3.78 (s, 3H), 1.54 (d, 3H) ppm; MS (ESI) m/z: 482 [M+Na]+.