反応 #68806

反応方程式

Water

4-(4-chloro-pyrimidin-2-yl)-morpholine

(S)—N-{1-[4-(3-hydroxy-azetidin-1-yl)-phenyl]-ethyl}-acetamide

NaH

→

desired product

(S)—N-(1-{4-[3-(2-Morpholin-4-yl-pyrimidin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamide

溶媒

DMF

DMF

反応条件

後処理

1. 1
   濃縮the mixture is concentrated in vacuo
2. 2
   その他the residue is purified by HPLC (XBridge, acetronitrile/H2O (+0.1% NH4OH))

実験手順

To 30 mg (0.15 mmol) 4-(4-chloro-pyrimidin-2-yl)-morpholine in DMF (1.0 mL) is added 30 mg (0.13 mmol) (S)—N-{1-[4-(3-hydroxy-azetidin-1-yl)-phenyl]-ethyl}-acetamide (V.1) in DMF (1.0 mL). 20 mg (0.45 mmol, 55% in mineral oil) NaH is added and the mixture is stirred for 12 h at room temperature. Water is added, the mixture is concentrated in vacuo and the residue is purified by HPLC (XBridge, acetronitrile/H2O (+0.1% NH4OH)) to yield the desired product.

出典