反応 #1985646

ord-2525a1a9dd04425ab41e7bb6d62e1cf7

反応方程式

COC(=O)c1cc2nc(Nc3c(Cl)cncc3Cl)[nH]c2c2c1OC(C)(C)C2
methyl 2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxylate
Nc1cc(F)c(F)cc1F
2,4,5-trifluoroaniline
[CH3][Al]([CH3])[CH3]
trimethyl aluminium
CC1(C)Cc2c(c(C(=O)Nc3cc(F)c(F)cc3F)cc3nc(Nc4c(Cl)cncc4Cl)[nH]c23)O1
desired product
収率 65.7%
CC1(C)Cc2c(c(C(=O)Nc3cc(F)c(F)cc3F)cc3nc(Nc4c(Cl)cncc4Cl)[nH]c23)O1
2-((3,5-Dichloropyridin-4-yl)amino)-7,7-dimethyl-N-(2,4,5-trifluorophenyl)-7,8-dihydro-1H-benzofuro[4,5-d]imidazole-5-carboxamide
収率 65.7%

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他The title compound was prepared
  2. 2
    その他at room temperature

実験手順

The title compound was prepared following the procedure described for Example-137 by using methyl 2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxylate (Step-1 of Intermediate-3, 0.250 g, 0.612 mmol), 2,4,5-trifluoroaniline (0.132 g, 0.9025 mmol), trimethyl aluminium (2M solution in toluene) (0.5 mL), dry toluene (10.0 mL) at room temperature to afford 0.210 g of the desired product. 1HNMR (DMSO-d6): δ 1.55 (s, 6H), 3.09 (s, 2H), 7.28 (s, 1H), 7.73 (q, J=10.2 Hz, 10.2 Hz, 1H), 8.43 (m, 3H), 10.02 (s, 1H), 11.00 (br s, 1H), 11.48 (br s, 1H); MS [M]+: 522.00.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08519149B2uspto-grants-2013_08