Trifluoroacetic acid → 4,7-Dichloro-1,2-dihydropyrrolo[3,4-c]pyridine-3-one

HRID 21342노트

반응식

HRID 21342 반응식
[Cl:1][C:2]1[C:7]2[C:8](=[O:21])[N:9](C(C)(C3C=CC=CC=3)C)[CH:10](O)[C:6]=2[C:5]([Cl:22])=[CH:4][N:3]=1.FC(F)(F)C(O)=O.C([SiH](CC)CC)C.CCCCCC.C(OCC)(=O)C>[N+](C)([O-])=O>[Cl:1][C:2]1[C:7]2[C:8](=[O:21])[NH:9][CH2:10][C:6]=2[C:5]([Cl:22])=[CH:4][N:3]=1

참가 물질

6

반응물 4

HCID 6422Trifluoroacetic acidHCID 12052TriethylsilaneHCID 21226206Ethyl acetate hexaneHCID 866283394,7-Dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one

생성물 1

HCID 768481314,7-Dichloro-1,2-dihydropyrrolo[3,4-c]pyridine-3-one수율 72%

시약·촉매·용매 1

HCID 6375Nitromethane용매

실험 절차

in a similar manner to Step 4 of Example 16, 4,7-dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one (38.8 mg, 0.115 mmol) was dissolved in nitromethane (1.6 mL), and the solution was treated with trifluoroacetic acid (0.177 mL, 2.30 mmol) and triethylsilane (55.1 mL, 0.345 mmol), followed by purification by slurry using chloroform/methanol and by preparative thin-layer chromatography (hexane/ethyl acetate=1/1) to obtain 4,7-dichloro-1,2-dihydropyrrolo[3,4-c]pyridine-3-one (16.8 mg, yield 72%).

후처리

  1. customfollowed by purification by slurry

출처 및 근거

ORD 기록
ord-a6f2ceabf1f34466a72d6dc411d700eb
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07745641B2

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