反応 #598373

ord-ee454f68f6a94f9886fdaa54e7967d67

反応方程式

O
Water
CC(C)(C)OC(=O)N1CCC(N)CC1
4-amino-piperidine-1-carboxylic acid tert-butyl ester
N#Cc1ccc(F)cc1C(F)(F)F
4-fluoro-2-trifluoromethyl-benzonitrile
O=C([O-])[O-].[K+].[K+]
potassium carbonate
CC(C)(C)OC(=O)N1CCC(Nc2ccc(C#N)c(C(F)(F)F)c2)CC1
desired compound
収率 68.0%
CC(C)(C)OC(=O)N1CCC(Nc2ccc(C#N)c(C(F)(F)F)c2)CC1
4-(4-cyano-3-trifluoromethyl-phenylamino)-piperidine-1-carboxylic acid tert-butyl ester
収率 68.0%

反応条件

温度
100°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他the precipitate formed
  2. 2
    その他is collected

実験手順

A mixture of 4-amino-piperidine-1-carboxylic acid tert-butyl ester (200 mg; 1.0 mmol), 4-fluoro-2-trifluoromethyl-benzonitrile (208 mg; 1.01 mmol) and potassium carbonate (276 mg; 2.0 mmol) in dimethylsulfoxide (3 mL) is heated to 100° C. over night. Water is then added and the precipitate formed is collected to afford the desired compound (250 mg; 0.68 mmol).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US09096524B2uspto-grants-2015_08