反応 #61784

反応方程式

water

sodium hydride

4-(4-[1,2,3]triazol-1-yl-butyl)-phenol

2-chloromethyl-6-(4-trifluoromethyl-phenyl)-pyridine

→

title compound

収率 60.3%

2-[4-(4-[1,2,3]triazol-1-yl-butyl)-phenoxymethyl]-6-(4-trifluoromethyl-phenyl)-pyridine

収率 60.3%

溶媒

N,N-dimethylformamide

反応条件

後処理

1. 1
   workup.STIRRINGstirring
2. 2
   workup.WAITcontinued at r.t for 2 days
3. 3
   workup.STIRRINGwas stirred for 1 h
4. 4
   その他the formed precipitate isolated by filtration
5. 5
   洗浄washed with water, methanol/water 1:1
6. 6
   その他The residue was dried at 40° C.

実験手順

16 mg (0.39 mmol) of 60% sodium hydride were added at 0° C. to a solution of 80 mg (0.37 mmol) 4-(4-[1,2,3]triazol-1-yl-butyl)-phenol in 4.0 ml N,N-dimethylformamide and stirred for 30 min. at 0° C. 100 mg (0.37 mmol) 2-chloromethyl-6-(4-trifluoromethyl-phenyl)-pyridine (WO 2004/007439) were given to the reaction mixture and stirring continued at r.t for 2 days. After addition of 8 ml water the mixture was stirred for 1 h, the formed precipitate isolated by filtration, washed with water, methanol/water 1:1, and a small amount of ether. The residue was dried at 40° C. to give 101 mg (60%) of the title compound as white powder.

出典