反応 #49261

反応方程式

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

収率 62.0%

溶媒

THF

反応条件

後処理

1. 1
   その他followed by purification by slurry
2. 2
   その他to obtain Compound BQ (177 mg, yield 62%)

実験手順

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%).

出典