Ethanol → HCID 86606527, compound
Reaction equation
[NH:1]1[CH2:6][CH2:5][CH:4]([CH2:7][NH:8][C:9](=[O:29])[CH:10]([C:22]2[CH:27]=[CH:26][CH:25]=[CH:24][C:23]=2[F:28])[NH:11][C:12]([NH:14][C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][CH:16]=2)=[O:13])[CH2:3][CH2:2]1.Cl.[C:31](=[NH:36])([O:33]CC)[CH3:32].CC[OH:39]>>[C:32]1(=[O:39])[N:36]([N:1]2[CH2:6][CH2:5][CH:4]([CH2:7][NH:8][C:9](=[O:29])[CH:10]([C:22]3[CH:27]=[CH:26][CH:25]=[CH:24][C:23]=3[F:28])[NH:11][C:12]([NH:14][C:15]3[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][CH:16]=3)=[O:13])[CH2:3][CH2:2]2)[C:31]1=[O:33]Participants
4
Procedure
A solution of N-(piperidin-4-ylmethyl)-2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide (from EXAMPLE 53, 70 mg, 0.17 mmol), ethyl acetimidate hydrochloride (40 mg, 0.32 mmol) and TEA (0.070 mL, 0.50 mmol) in EtOH (3 mL) was stirred at room temperature overnight. It was then concentrated in vacuo. The residue was purified by HPLC to give the titled compound as a white powder (37 mg). MS 460.1 and 462.1 (M+H, Cl pattern).