تفاعل #1603331

معادلة التفاعل

2-(benzyloxy)-6-bromopyridine

toluene

sodium t-butoxide

pyrrolidine

→

2-(benzyloxy)-6-(pyrrolidin-1-yl)pyridine

المردود 92.4%

المذيبات

ethyl acetate

ظروف التفاعل

المعالجة

1. 1
   workup.ADDITIONIn a dried microwave reactor into which an argon gas was introduced
2. 2
   أخرىat 120° C.
3. 3
   أخرىfor 10 min
4. 4
   ترشيحfiltered through Cellite
5. 5
   أخرىto remove the solvent

الإجراء التجريبي

In a dried microwave reactor into which an argon gas was introduced, 526 mg (2.0 mmol) of 2-(benzyloxy)-6-bromopyridine, 200 μl (2.4 mmol) of pyrrolidine, 283 mg (2.8 mmol) of sodium t-butoxide, 9 mg (0.005 mmol) of tris(dibenzylideneacetone)dipalladium(0) (0.5 mol % of Pd), 19 mg (0.015 mmol, 1.5 mol %) of (±)-BINAP and 3 ml of toluene were placed, followed by stirring and reacting the mixture using microwave at 120° C. for 10 min. The reaction mixture was diluted with 20 ml of ethyl acetate, filtered through Cellite, and kept under a reduced pressure to remove the solvent. The residue was subjected to column chromatography using 10% ethyl acetate/hexane as an eluent to obtain 470 mg (yield 92%) of 2-(benzyloxy)-6-(pyrrolidin-1-yl)pyridine.

المصدر