N-(2-fluoro-4-nitrobenzyl)methanesulfonamide → N-(4-amino-2-fluorobenzyl)methanesulfonamide

HRID 1428739ノート

反応式

HRID 1428739 の反応式
[F:1][C:2]1[CH:13]=[C:12]([N+:14]([O-])=O)[CH:11]=[CH:10][C:3]=1[CH2:4][NH:5][S:6]([CH3:9])(=[O:8])=[O:7]>O1CCCC1.C(O)C.[Pd]>[NH2:14][C:12]1[CH:11]=[CH:10][C:3]([CH2:4][NH:5][S:6]([CH3:9])(=[O:8])=[O:7])=[C:2]([F:1])[CH:13]=1

参加物

5

反応物 1

HCID 86679366N-(2-fluoro-4-nitrobenzyl)methanesulfonamide

生成物 1

HCID 86679367N-(4-amino-2-fluorobenzyl)methanesulfonamide収率 86.5%

試薬・触媒・溶媒 3

HCID 23938Palladium触媒HCID 702Ethanol溶媒HCID 8028Tetrahydrofuran溶媒

実験手順

To a stirred solution of N-(2-fluoro-4-nitrobenzyl)methanesulfonamide (250 mg, 1.007 mmol) in tetrahydrofuran and ethanol as co-solvent were added 10% Pd/C (25 mg). The mixture was charged with H2 (gas) balloon. The resulting mixture was stirred for 15 h, then filtered by using celite. The filtrate was removed in vacuo. The crude was purified by column chromatography. N-(4-Amino-2-fluorobenzyl)methanesulfonamide (190 mg) was obtained as 86% yield.

後処理

  1. additionThe mixture was charged with H2 (gas) balloon
  2. filtrationfiltered
  3. customThe filtrate was removed in vacuo
  4. customThe crude was purified by column chromatography

出典と根拠

ORDレコード
ord-17862222d0ab44c58a5ceb989df33303
出典データセット
uspto-grants-2015_01
特許番号
US08937092B2

反応ノート

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