5-Fluoro-3-pyridinamine → HCID 68227175, Verbindung

HRID 403260

Reaktionsgleichung

Reaktionsgleichung von HRID 403260
Br[C:2]1[CH:3]=[CH:4][C:5]([F:21])=[C:6]([C@:8]2([CH3:20])[C:14]([F:16])([F:15])[C:13]([CH3:18])([CH3:17])[O:12][CH2:11][C:10](=[O:19])[NH:9]2)[CH:7]=1.[NH2:22][C:23]1[CH:24]=[N:25][CH:26]=[C:27]([F:29])[CH:28]=1>>[F:15][C:14]1([F:16])[C:13]([CH3:18])([CH3:17])[O:12][CH2:11][C:10](=[O:19])[NH:9][C@@:8]1([C:6]1[CH:7]=[C:2]([NH:22][C:23]2[CH:24]=[N:25][CH:26]=[C:27]([F:29])[CH:28]=2)[CH:3]=[CH:4][C:5]=1[F:21])[CH3:20]

Komponenten

3

Edukt 2

HCID 5744505-Fluoro-3-pyridinamineHCID 58562968(R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-one

Produkt 1

HCID 68227175HCID 68227175, VerbindungAusbeute 26 %

Versuchsvorschrift

Prepared in an analogous manner as described for intermediate A9A or A13A from (R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-one (intermediate A16B) (200 mg, 546 μmol) and commercially available 3-amino-5-fluoropyridine [CAS no 210169-05-4] (122 mg, 1.09 mmol). The (R)-6,6-difluoro-5-(2-fluoro-5-(5-fluoropyridin-3-ylamino)phenyl)-5,7,7-trimethyl-1,4-oxazepan-3-one (56 mg, 26%) was obtained as an off-white foam. MS (ISP): m/z=398.2 [(M+H)+].

Aufarbeitung

  1. customPrepared in an analogous manner

Quellen und Nachweise

ORD-Eintrag
ord-db8bbf54e5174e408e2140a1fa0cffc6
Quelldatensatz
uspto-grants-2014_06
Patentnummer
US08748418B2

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