反応 #2166327

反応方程式

4-(5-methyl-[1,2,4]oxadiazol-3-yl)phenylamine

8-methoxychromane-6-carbaldehyde

1g

2-{3-[(4-carbamimidoylphenylamino)-(2-fluoro-4,5-dimethoxyphenyl)methyl]5-oxo-4,5-dihydro-[1,2,4]triazol-1-yl}benzoic Acid trifluoroacetate

trimethylsilyl cyanide

Yb(OTf)3

→

(8-methoxychroman-6-yl)-[4-(5-methyl-[1,2,4]oxadiazol-3-yl)phenylamino]acetonitrile

溶媒

dichloromethane

反応条件

後処理

1. 1
   ろ過The reaction mixture was filtered through celite
2. 2
   洗浄the celite was washed with 100 ml of ethyl acetate
3. 3
   濃縮The organic layer was concentrated under reduced pressure

実験手順

After adding 700 mg of 4-(5-methyl-[1,2,4]oxadiazol-3-yl)phenylamine, 770 mg of 8-methoxychromane-6-carbaldehyde [CAS No. 81258-23-3], 1g of MS3A and 1.1 ml of trimethylsilyl cyanide to a solution of 250 mg of Yb(OTf)3 in 5 ml of dichloromethane under a nitrogen atmosphere, the mixture was stirred overnight at room temperature. The reaction mixture was filtered through celite, and the celite was washed with 100 ml of ethyl acetate. The organic layer was concentrated under reduced pressure to give a crude product of (8-methoxychroman-6-yl)-[4-(5-methyl-[1,2,4]oxadiazol-3-yl)phenylamino]acetonitrile.

出典