Aspirin → 2-hydroxy-N-(2-(4-(isopropylsulfonyl)phenyl)-5-trityl-5H-pyrrolo[2,3-b]pyrazin-7-yl)benzamide

HRID 68666

반응식

HRID 68666 반응식
C([O:4][C:5]1[CH:13]=[CH:12][CH:11]=[CH:10][C:6]=1[C:7]([OH:9])=O)(=O)C.[CH:14]([S:17]([C:20]1[CH:25]=[CH:24][C:23]([C:26]2[N:27]=[C:28]3[C:34]([NH2:35])=[CH:33][N:32]([C:36]([C:49]4[CH:54]=[CH:53][CH:52]=[CH:51][CH:50]=4)([C:43]4[CH:48]=[CH:47][CH:46]=[CH:45][CH:44]=4)[C:37]4[CH:42]=[CH:41][CH:40]=[CH:39][CH:38]=4)[C:29]3=[N:30][CH:31]=2)=[CH:22][CH:21]=1)(=[O:19])=[O:18])([CH3:16])[CH3:15].CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.[B-](F)(F)(F)F.CN1CCOCC1>C(Cl)Cl>[OH:4][C:5]1[CH:13]=[CH:12][CH:11]=[CH:10][C:6]=1[C:7]([NH:35][C:34]1[C:28]2[C:29](=[N:30][CH:31]=[C:26]([C:23]3[CH:24]=[CH:25][C:20]([S:17]([CH:14]([CH3:16])[CH3:15])(=[O:19])=[O:18])=[CH:21][CH:22]=3)[N:27]=2)[N:32]([C:36]([C:49]2[CH:50]=[CH:51][CH:52]=[CH:53][CH:54]=2)([C:43]2[CH:44]=[CH:45][CH:46]=[CH:47][CH:48]=2)[C:37]2[CH:42]=[CH:41][CH:40]=[CH:39][CH:38]=2)[CH:33]=1)=[O:9]

참가 물질

6

반응물 4

HCID 2244AspirinHCID 79724-MethylmorpholineHCID 2733207O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 711435912-(4-Isopropylsulfonylphenyl)-5-trityl-pyrrolo[2,3-b]pyrazin-7-amine

생성물 1

HCID 711549822-hydroxy-N-(2-(4-(isopropylsulfonyl)phenyl)-5-trityl-5H-pyrrolo[2,3-b]pyrazin-7-yl)benzamide

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

A 5 mL microwave vial was charged with 2-acetoxybenzoic acid (33.87 mg, 0.1880 mmol) To this was added a solution of 2-(4-isopropylsulfonylphenyl)-5-trityl-pyrrolo[2,3-b]pyrazin-7-amine (100 mg, 0.1790 mmol), TBTU in DCM (1 mL) followed by PS-NMM. The reaction was shaken for 3 hours at ambient temperature then filtered and the resin washed with DCM (1 mL). This crude mixture was taken onto the next step as is.

후처리

  1. filtrationthen filtered
  2. washthe resin washed with DCM (1 mL)

출처 및 근거

ORD 기록
ord-b41611152f6444abbee94ae2e2d8366d
출처 데이터셋
uspto-grants-2014_09
특허 번호
US08822469B2

연결된 노트

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