Trifluoroacetic acid → (S)-2-Amino-3-(4-iodophenyl)propanamide

HRID 216902ノート

反応式

HRID 216902 の反応式
[NH2:1][C:2](=[O:20])[C@@H:3]([NH:12]C(=O)OC(C)(C)C)[CH2:4][C:5]1[CH:10]=[CH:9][C:8]([I:11])=[CH:7][CH:6]=1.FC(F)(F)C(O)=O>ClCCl>[NH2:12][C@@H:3]([CH2:4][C:5]1[CH:6]=[CH:7][C:8]([I:11])=[CH:9][CH:10]=1)[C:2]([NH2:1])=[O:20]

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 57999635(S)-tert-Butyl (1-amino-3-(4-iodophenyl)-1-oxopropan-2-yl)carbamate

生成物 1

HCID 447705(S)-2-Amino-3-(4-iodophenyl)propanamide

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

(S)-tert-Butyl 1-amino-3-(4-iodophenyl)-1-oxopropan-2-ylcarbamate (Example 1, step (i), 2.41 g) was stirred in dichloromethane (125 mL) and to the suspension was added trifluoroacetic acid (8 mL). The mixture was stirred for 2 h and then concentrated to ˜12 mL in vacuo. The residue was stirred for 2 days, dissolved in ethyl acetate/dichloromethane and washed with water containing an excess of sodium bicarbonate. The organic layer was dried and evaporated to the sub-titled compound (1.52 g).

後処理

  1. concentrationconcentrated to ˜12 mL in vacuo
  2. stirringThe residue was stirred for 2 days
  3. dissolutiondissolved in ethyl acetate/dichloromethane
  4. washwashed with water containing an excess of sodium bicarbonate
  5. customThe organic layer was dried
  6. customevaporated to the sub-titled compound (1.52 g)

出典と根拠

ORDレコード
ord-d85c8daa8e99494ea7e46176865567d7
出典データセット
uspto-grants-2012_06
特許番号
US08193239B2

反応ノート

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