Trifluoroacetic acid → 8-Chloro-4-[3-(2-methyl-oxazol-4-yl)-phenyl]-7-(methyl-propyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

HRID 1265928Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1265928
C(OC(=O)[NH:7][C:8]1[CH:13]=[C:12]([N:14]([CH3:18])[CH2:15][CH2:16][CH3:17])[C:11]([Cl:19])=[CH:10][C:9]=1[NH2:20])(C)(C)C.C(O[C:27](=[O:43])[CH2:28][C:29](=O)[C:30]1[CH:35]=[CH:34][CH:33]=[C:32]([C:36]2[N:37]=[C:38]([CH3:41])[O:39][CH:40]=2)[CH:31]=1)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[Cl:19][C:11]1[C:12]([N:14]([CH3:18])[CH2:15][CH2:16][CH3:17])=[CH:13][C:8]2[N:7]=[C:29]([C:30]3[CH:35]=[CH:34][CH:33]=[C:32]([C:36]4[N:37]=[C:38]([CH3:41])[O:39][CH:40]=4)[CH:31]=3)[CH2:28][C:27](=[O:43])[NH:20][C:9]=2[CH:10]=1

Komponenten

5

Edukt 3

HCID 6422Trifluoroacetic acidHCID 69688379Carbamic acid,[2-amino-4-chloro-5-(methylpropylamino)phenyl]-,1,1-dimethylethyl esterHCID 696892093-Oxo-3-[3-(2-methyl-oxazol-4-yl)-phenyl]-propionic acid tert-butyl ester

Produkt 1

HCID 186134428-Chloro-4-[3-(2-methyl-oxazol-4-yl)-phenyl]-7-(methyl-propyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Versuchsvorschrift

The title compound was prepared from [2-amino-4-chloro-5-(methyl-propyl-amino)-phenyl]-carbamic acid tert-butyl ester (0.16 g) (Example J8) and 3-oxo-3-[3-(2-methyl-oxazol-4-yl)-phenyl]-propionic acid tert-butyl ester (0.17 g) (Example K29) according to the general procedure M. The obtained material was deprotected and cyclized by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a yellow solid (0.07 g).

Quellen und Nachweise

ORD-Eintrag
ord-bf5bbb09caa14875ae728843771287ad
Quelldatensatz
uspto-grants-2003_04
Patentnummer
US06544985B2

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