1-Hydroxybenzotriazole → HCID 178496719、化合物

反応式

[NH2:1][C@H:2]1[CH2:7][CH2:6][N:5]([C:8]([O:10][C:11]([CH3:14])([CH3:13])[CH3:12])=[O:9])[CH2:4][C@H:3]1[O:15][CH3:16].[F:17][C:18]([F:28])([F:27])[C:19]1[N:20]=[C:21]([C:24](O)=[O:25])[NH:22][CH:23]=1.CCN=C=NCCCN(C)C.Cl.C1C=CC2N(O)N=NC=2C=1>>[F:28][C:18]([F:17])([F:27])[C:19]1[N:20]=[C:21]([C:24]([NH:1][C@H:2]2[CH2:7][CH2:6][N:5]([C:8]([O:10][C:11]([CH3:12])([CH3:13])[CH3:14])=[O:9])[CH2:4][C@H:3]2[O:15][CH3:16])=[O:25])[NH:22][CH:23]=1

参加物

反応物 4

HCID 757711-Hydroxybenzotriazole

HCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride

HCID 57362389(3R,4S)-4-Amino-1-boc-3-methoxypiperidine2 回

HCID 178524893HCID 178524893、化合物

生成物 1

HCID 178496719HCID 178496719、化合物

実験手順

The same operation as in Example (1g) was performed using tert-butyl cis(±)-4-amino-3-methoxypiperidine-1-carboxylate obtained by the method described in Example (1e) (0.90 g, 3.91 mmol), 4-(trifluoromethyl)-1H-imidazole-2-carboxylic acid obtained in Example (33c) (0.40 g, 2.22 mmol), WSC hydrochloride (1.25 g, 6.52 mmol) and HOBT (0.30 g, 2.22 mmol), to obtain 0.67 g of the title compound as a white foamy substance (77%).