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

반응식

HRID 10973 반응식
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

참가 물질

4

반응물 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

생성물 1

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

시약·촉매·용매 1

HCID 962Water촉매

실험 절차

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.

후처리

  1. concentrationThe mixture was concentrated in vacuo

출처 및 근거

ORD 기록
ord-87b4f71a3c464d95bdbbcf9b03be006a
출처 데이터셋
uspto-grants-2006_08
특허 번호
US07094783B2

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