Reacción #49261

Ecuación de reacción

5-[1-(tert-butoxycarbonyl)-4-piperidyl-N-(tert-butoxycarbonyl)amino]-1-(tert-butoxycarbonyl)indole

triisopropyl borate

LDA heptane THF ethylbenzene

→

5-[1-(tert-butoxycarbonyl)-4-piperidylamino]indole

Rendimiento 62.0%

Disolventes

THF

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrofollowed by purification by slurry
2. 2
   Otroto obtain Compound BQ (177 mg, yield 62%)

Procedimiento

In a similar manner to Step 2 of Reference Example 1, 5-[1-(tert-butoxycarbonyl)-4-piperidyl-N-(tert-butoxycarbonyl)amino]-1-(tert-butoxycarbonyl)indole (320 mg, 0.621 mmol) was dissolved in THF (5 mL), and the solution was treated with triisopropyl borate (0.215 mL, 0.932 mmol) and LDA-heptane/THF/ethylbenzene solution (2.0 mol/L, 0.776 mL, 1.55 mmol), followed by purification by slurry using hexane to obtain Compound BQ (177 mg, yield 62%).

Fuente