反応 #2345

反応方程式

compound

Methyl 2-t-butoxycarbonylamino-4-[4-[4-(4-pyridyl)-piperazin-1-yl]phenoxy]butyrat

→

title compound

収率 74.1%

Methyl 2-amino-4-[4-[4-(4-pyridyl) piperazin-1-yl]-phenoxy]butyrate

収率 74.1%

溶媒

TFA

反応条件

後処理

1. 1
   その他The solution was evaporated
2. 2
   workup.DISSOLUTIONthe residue dissolved in water (15 ml)
3. 3
   抽出The mixture was extracted three times with dichloromethane
4. 4
   その他Evaporation of the combined extracts

実験手順

The compound of Example 140 (0.96 g) in TFA (10 ml) was kept at room temperature for 2 hours. The solution was evaporated and the residue dissolved in water (15 ml) and the solution basified with sodium carbonate. The mixture was extracted three times with dichloromethane. Evaporation of the combined extracts gave the title compound (0.56 g); m.p. 125°-127° C.; NMR(d6DMSO) δ 8.2(2H,d), 6.92(6H,m), 4.0(2H,m), 3.64(3H,s), 3.46(4H,t), 3.15(4H,t), 2.04(2H,m), 1.84(1H, m); m/e 371(M+H)+. Calculated for C20H26N4 O3. 0.75 H2O: C, 62.5; H, 7.17; N, 14.6. Found: C, 62.8; H, 6.8; N, 14.3%.

出典