Reaktion #10667

Reaktionsgleichung

Intermediate 121

trans-N-(tert-butoxycarbonyl)-4-[(4-bromo-5-isoquinolyl)oxy]cyclohexylamine

2-(di-tert-butylphosphino)biphenyl

sodium tert-butoxide

ammonia dioxane

→

title compound

trans-N-(tert-butoxycarbonyl)-4-[(4-amino-5-isoquinolyl)oxy]cyclohexylamine

Reaktionsbedingungen

Aufarbeitung

1. 1
   FiltrationThe reaction mixture was filtered through a Celite layer
2. 2
   Sonstigethe solvent was evaporated under reduced pressure
3. 3
   SonstigeThen, the residue was purified by silica gel column chromatography (chloroform:methanol=9:1)

Vorschrift

A suspension of Intermediate 121 (100 mg), tris(dibenzylideneacetone)dipalladium(0) (22.1 mg), 2-(di-tert-butylphosphino)biphenyl (33.9 mg) and sodium tert-butoxide (35.3 mg) in 0.5 N ammonia/dioxane solution (2 ml) was stirred at 70° C. for 22 hours. The reaction mixture was filtered through a Celite layer, and the solvent was evaporated under reduced pressure. Then, the residue was purified by silica gel column chromatography (chloroform:methanol=9:1) to obtain the title compound (36.1 mg).

Quelle