Triethylamine → HCID 178474444、化合物

HRID 1360896ノート

反応式

HRID 1360896 の反応式
[C:1]([NH:4][C:5]1[S:6][C:7]([C:11]2[CH:12]=[C:13]([S:17](Cl)(=[O:19])=[O:18])[S:14][C:15]=2[Br:16])=[C:8]([CH3:10])[N:9]=1)(=[O:3])[CH3:2].C(N(CC)CC)C.[NH2:28][C:29]1[NH:33][N:32]=[N:31][N:30]=1>C(Cl)Cl>[Br:16][C:15]1[S:14][C:13]([S:17](=[O:19])(=[O:18])[NH:28][C:29]2[NH:33][N:32]=[N:31][N:30]=2)=[CH:12][C:11]=1[C:7]1[S:6][C:5]([NH:4][C:1](=[O:3])[CH3:2])=[N:9][C:8]=1[CH3:10]

参加物

5

反応物 3

HCID 8471TriethylamineHCID 866231464-[2-(Acetylamino)-4-methyl-1,3-thiazol-5-yl]-5-bromothiophene-2-sulfonylchlorideHCID 178509299HCID 178509299、化合物

生成物 1

HCID 178474444HCID 178474444、化合物収率 64%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

4-[2-(acetylamino)-4-methyl-1,3-thiazol-5-yl]-5-bromothiophene-2-sulfonyl chloride, prepared as in Step III of Example 23 (500 mg; 1.2 mmol; 1 eq), is dissolved in anhydrous DCM (30 ml). The reaction is put under nitrogen. Triethylamine (0.34 ml; 2.41 mmol; 2 eq) and 5-amino-1H-tetrazole (204.6 mg; 2.41 mmol; 2 eq) are added successively and the reaction mixture is stirred overnight at room temperature. It is then washed with water, NH4Cl sat., brine and dried over MgSO4, affording the title compound (550 mg; 64%).

後処理

  1. washIt is then washed with water, NH4Cl sat., brine
  2. dry with materialdried over MgSO4

出典と根拠

ORDレコード
ord-95de6a396a57436382b5451341ebb008
出典データセット
uspto-grants-2011_02
特許番号
US07879888B2

反応ノート

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