4-Methylmorpholine → (S)-2-{4'-[4-(4-Methanesulfonyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl}-azetidine-1-carboxylic acid tert-butyl ester

HRID 1678504Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1678504
[C:1]([O:5][C:6]([N:8]1[CH2:11][CH2:10][C@H:9]1[C:12](=[O:34])[NH:13][C:14]1[CH:15]=[C:16]([C:25]2[CH:30]=[CH:29][C:28]([C:31]([OH:33])=O)=[CH:27][CH:26]=2)[C:17]([O:20][C:21]([F:24])([F:23])[F:22])=[CH:18][CH:19]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[CH3:35][S:36]([N:39]1[CH2:44][CH2:43][N:42]([CH2:45][C:46]2[CH:51]=[CH:50][C:49]([NH2:52])=[CH:48][CH:47]=2)[CH2:41][CH2:40]1)(=[O:38])=[O:37].CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.CN1CCOCC1>CN(C=O)C.O>[C:1]([O:5][C:6]([N:8]1[CH2:11][CH2:10][C@H:9]1[C:12](=[O:34])[NH:13][C:14]1[CH:15]=[C:16]([C:25]2[CH:26]=[CH:27][C:28]([C:31](=[O:33])[NH:52][C:49]3[CH:50]=[CH:51][C:46]([CH2:45][N:42]4[CH2:41][CH2:40][N:39]([S:36]([CH3:35])(=[O:38])=[O:37])[CH2:44][CH2:43]4)=[CH:47][CH:48]=3)=[CH:29][CH:30]=2)[C:17]([O:20][C:21]([F:23])([F:22])[F:24])=[CH:18][CH:19]=1)=[O:7])([CH3:3])([CH3:2])[CH3:4]

Komponenten

7

Edukt 4

HCID 79724-MethylmorpholineHCID 2733084Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 113692314-(4-Methanesulfonyl-piperazin-1-ylmethyl)-phenylamineHCID 67374213(S)-2-(4'-Carboxy-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl)-azetidine-1-carboxylic acid tert-butyl ester

Produkt 1

HCID 67372397(S)-2-{4'-[4-(4-Methanesulfonyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl}-azetidine-1-carboxylic acid tert-butyl ester

Reagenzien, Katalysatoren, Lösungsmittel 2

HCID 962WaterLösungsmittelHCID 6228DimethylformamideLösungsmittel

Versuchsvorschrift

A mixture of (S)-2-(4′-Carboxy-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl)-azetidine-1-carboxylic acid tert-butyl ester (50 mg), 4-(4-methanesulfonyl-piperazin-1-ylmethyl)-phenylamine (29 mg), HBTU (61 mg) and N-methyl morpholine (0.033 ml) in dry DMF (3 ml) was stirred at room temp for 18 h. Water (10 ml) was then added and the cream solid collected by filtration and used without purification or characterisation.

Aufarbeitung

  1. filtrationthe cream solid collected by filtration
  2. customused without purification or characterisation

Quellen und Nachweise

ORD-Eintrag
ord-38e48f92abae4795bad99f7a41f92f08
Quelldatensatz
uspto-grants-2011_08
Patentnummer
US08008303B2

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