反応式
NS(C1C=CC(CCN[C:14]([C:16]2[CH:21]=[N:20][C:19]([CH3:22])=[CH:18][N:17]=2)=[O:15])=CC=1)(=O)=O.CC1N=CC([C:30](O)=[O:31])=NC=1>CO>[CH3:30][O:31][C:14]([C:16]1[CH:21]=[N:20][C:19]([CH3:22])=[CH:18][N:17]=1)=[O:15]参加物
実験手順
A process for the preparation of N-[2-[4-(aminosulfonyl)phenyl]ethyl]-5-methylpyrazine-carboxamide of the formula I: ##STR21## consisting of: i) treating 5-methylpyrazine-2-carboxylic acid of the formula VIII: ##STR22## with methanol under reflux to obtain 5-methylpyrazine-2-carboxylic acid methyl ester of the formula VIII A: ##STR23## ii) reacting 5-methylpyrazine-2-carboxylic acid methyl ester of the formula VIII A with 2-phenylethylamine of the formula II: ##STR24## at 100° to 200° C. to obtain 5-methylpyrazine 2-(2-phenylethyl) carboxamide of the formula IX: ##STR25## iii) chlorosulfonating the 5-methylpyrazine-2-(2-phenylethyl)carboxamide of the formula IX with chlorosulfonic acid at 0°-45° C. to obtain [N-[2-[4-(chlorosulfonyl)phenyl]ethyl]-5-methylpyrazine carboxamide] of the formula X: ##STR26## iv) and treating the [N-[2-[4-(chlorosulfonyl)phenyl]ethyl]-5-methyl purazinecarboxamide] of the formula X with ammonia to obtain N-[2-[4-(aminosulfonyl)phenyl]ethyl]-5-methylpyrazine carboxamide of the formula I.
出典と根拠
- ORDレコード
- ord-d948403bfd334ae58c8b8f8b1f3c072b
- 出典データセット
- uspto-grants-1996_05
- 特許番号
- US05516906
関連ノート
読み込み中…