Reaction #2264798

Reaction equation

product

(2,3-dichloro-4-fluorophenyl)(4-methyl-1-(pyrazin-2-yl)-1H-[1,2,3]triazolo[4,5-c]pyridin-5(4H)-yl)methanone

triethylsilane

→

title compound

Yield 40.0%

(2,3-dichloro-4-fluorophenyl)(4-methyl-1-(pyrazin-2-yl)-6,7-dihydro-1H-[1,2,3]triazolo[4,5-c]pyridin-5(4H)-yl)methanone

Yield 40.0%

Solvents

CH2Cl2

TFA

Conditions

Workup

1. 1
   OtherThe reaction was sealed
2. 2
   Washthe organic portion washed with NaHCO3
3. 3
   DryingThe organic portion was then dried over Na2SO4
4. 4
   Concentrationconcentrated
5. 5
   Otherpurified by chromatography on silica gel
6. 6
   Washeluted with heptane/EtOAc

Procedure

To a solution of the product of Example 140, Step 1 (350 mg, 0.864 mmol) in TFA (2 mL) was added triethylsilane (0.35 mL, 2.16 mmol). The reaction was sealed and heated at 80° C. for 2 h. The reaction was diluted with CH2Cl2 and the organic portion washed with NaHCO3. The organic portion was then dried over Na2SO4, concentrated and purified by chromatography on silica gel eluted with heptane/EtOAc to afford the title compound (140 mg, 40%) MS (ESI) mass calcd. C17H13Cl2FN6O 406.1. m/z found, 407.0 [M+H]+.

Source