Reacción #9059

Ecuación de reacción

2,3-dihydrobenzofuran-7-carboxaldehyde

[1-(tert-butoxycarbonyl)-(1H-benzimidazol-2-ylmethyl)]-(5,6,7,8-tetrahydro-quinolin-8-yl)-amine

NaBH(OAc)3

→

(1H-Benzimidazol-2-ylmethyl)-(2,3-dihydro-benzofuran-7-ylmethyl)-(5,6,7,8-tetrahydro-quinolin-8-yl)-amine

Condiciones de reacción

Tratamiento posterior

1. 1
   OtroPurification of the crude product by radial chromatography on silica gel (1 mm TLC plate, 125:1:1 CH2Cl2:CH3OH:NH4OH)
2. 2
   Otroto gave the desired freebase (48 mg, 33%)

Procedimiento

Following General Procedure B: To a solution of 2,3-dihydrobenzofuran-7-carboxaldehyde (53.6 mg, 0.362 mmol) and [1-(tert-butoxycarbonyl)-(1H-benzimidazol-2-ylmethyl)]-(5,6,7,8-tetrahydro-quinolin-8-yl)-amine (136 mg, 0.361 mmol) CH2Cl2 (5 mL) was added NaBH(OAc)3 (112 mg, 0.528 mmol) and the mixture stirred overnight. Purification of the crude product by radial chromatography on silica gel (1 mm TLC plate, 125:1:1 CH2Cl2:CH3OH:NH4OH) to gave the desired freebase (48 mg, 33%).

Fuente