反应 #554653

反应方程式

1-4

(1-Benzylazepan-3-yl)methanol

3-methyl-4-fluorophenol

DIAD

→

1-5

1-Benzyl-3-[(4-fluoro-3-methylphenoxy)methyl]azepane

溶剂

DCM

反应条件

后处理

1. 1
   过滤filtered
2. 2
   浓缩the filtrate was concentrated
3. 3
   其他The crude material was purified by gradient elution on silica gel (0 to 50% EtOAc in Hex)

实验过程

A solution of 1-4 (500 mg, 2.280 mmol), 3-methyl-4-fluorophenol (288 mg, 2.280 mmol), and tiphenylphosphine-resin bound (1.060 g @ 2.15 mmol/g) in DCM (20 ml) was treated with DIAD (0.443 ml, 2.280 mmol). The mixture was stirred overnight at RT, filtered, and the filtrate was concentrated. The crude material was purified by gradient elution on silica gel (0 to 50% EtOAc in Hex) to yield 1-5 as a pale yellow oil. Data for 1-5: LRMS m/z (M+H): 328.2.

来源