Trifluoroacetic acid methylene chloride → 3-benzyloxycarbonylamino-6-methyl-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carboxylic Acid

HRID 10973

反応式

HRID 10973 の反応式
C([O:5][C:6]([C:8]1([CH3:29])[N:12]2[C:13](=[O:28])[C:14]([NH:17][C:18]([O:20][CH2:21][C:22]3[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=3)=[O:19])=[CH:15][N:16]=[C:11]2[CH2:10][CH2:9]1)=[O:7])(C)(C)C.C(O)(C(F)(F)F)=O.C(Cl)Cl>O>[CH2:21]([O:20][C:18]([NH:17][C:14]1[C:13](=[O:28])[N:12]2[C:8]([CH3:29])([C:6]([OH:7])=[O:5])[CH2:9][CH2:10][C:11]2=[N:16][CH:15]=1)=[O:19])[C:22]1[CH:23]=[CH:24][CH:25]=[CH:26][CH:27]=1

参加物

4

反応物 2

HCID 21863450Trifluoroacetic acid methylene chlorideHCID 696008793-benzyloxycarbonylamino-6-methyl-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carboxylic Acid tert-butyl Ester

生成物 1

HCID 219796983-benzyloxycarbonylamino-6-methyl-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carboxylic Acid収率 105.5%

試薬・触媒・溶媒 1

HCID 962Water触媒

実験手順

A solution of intermediate 19a (55 mg, 0.138 mmol) in 4 mL 1:1 TFA/CH2Cl2 with 2 drops water was stirred at rt for 12 h. The mixture was concentrated in vacuo, then coevaporated with CCl4 to afford 50 mg of intermediate 19b (quantitative), which was used without further purification in the following step.

後処理

  1. concentrationThe mixture was concentrated in vacuo

出典と根拠

ORDレコード
ord-87b4f71a3c464d95bdbbcf9b03be006a
出典データセット
uspto-grants-2006_08
特許番号
US07094783B2

関連ノート

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