Reaktion #10676

Reaktionsgleichung

Intermediate 84

4-(1-chloro-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine

4-methoxybenzylamine

2-(di-tert-butylphosphino)biphenyl

sodium tert-butoxide

→

title compound

4-[1-(4-methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine

Lösungsmittel

toluene

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 (n-hexane:ethyl acetate=3:1)

Vorschrift

A suspension of Intermediate 84 (235 mg), 4-methoxybenzylamine (110 μl), tris(dibenzylideneacetone)dipalladium(0) (30.4 mg), 2-(di-tert-butylphosphino)biphenyl (41.0 mg) and sodium tert-butoxide (93.6 mg) in toluene (4.5 ml) was stirred at 70° C. for 1 hour. 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 (n-hexane:ethyl acetate=3:1) to obtain the title compound (270 mg).

Quelle