3-(2-Butoxy-6-trifluoromethyl-pyridin-3-yl)-acrylic acid → 3-(2-Butoxy-6-trifluoromethyl-pyridin-3-yl)-N-(3-ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-acrylamide
Reaction equation
Cl.[NH2:2][CH2:3][C:4]1[CH:9]=[C:8]([F:10])[C:7]([NH:11][S:12]([CH3:15])(=[O:14])=[O:13])=[C:6]([C:16]#[CH:17])[CH:5]=1.[CH2:18]([O:22][C:23]1[C:28]([CH:29]=[CH:30][C:31](O)=[O:32])=[CH:27][CH:26]=[C:25]([C:34]([F:37])([F:36])[F:35])[N:24]=1)[CH2:19][CH2:20][CH3:21]>>[CH2:18]([O:22][C:23]1[C:28]([CH:29]=[CH:30][C:31]([NH:2][CH2:3][C:4]2[CH:9]=[C:8]([F:10])[C:7]([NH:11][S:12]([CH3:15])(=[O:14])=[O:13])=[C:6]([C:16]#[CH:17])[CH:5]=2)=[O:32])=[CH:27][CH:26]=[C:25]([C:34]([F:37])([F:35])[F:36])[N:24]=1)[CH2:19][CH2:20][CH3:21]Participants
3
Procedure
N-(4-Aminomethyl-2-ethynyl-6-fluoro-phenyl)-methanesulfonamide HCl salt (25 mg, 0.087 mmol) was reacted with 3-(2-butoxy-6-trifluoromethyl-pyridin-3-yl)-acrylic acid (21 mg, 0.73 mmol) to give the title compound (24 mg, 54%).