1-(tert-Butoxycarbonyl)-4-(methanesulfonyloxy)piperidine → 4-[4-Fluoro-1-(2-fluoro-phenyl)-1H-indazol-3-yloxy]-piperidine-1-carboxylic acid tert-butyl ester

HRID 30413

Reaktionsgleichung

Reaktionsgleichung von HRID 30413
[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][CH:11](OC2C3C(=CC=CC=3)N(C3C=CC(Cl)=CC=3)N=2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[F:31][C:32]1[CH:40]=[CH:39][CH:38]=[C:37]2[C:33]=1[C:34]([OH:48])=[N:35][N:36]2[C:41]1[CH:46]=[CH:45][CH:44]=[CH:43][C:42]=1[F:47].CCN(P1(N(CC2C=CC=CC=2)CCCN1C)=NC(C)(C)C)CC.C=CC1C=CC=CC=1.C=CC1C=CC(C=C)=CC=1.C(OC(N1CCC(OS(C)(=O)=O)CC1)=O)(C)(C)C>CN(C=O)C>[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][CH:11]([O:48][C:34]2[C:33]3[C:37](=[CH:38][CH:39]=[CH:40][C:32]=3[F:31])[N:36]([C:41]3[CH:46]=[CH:45][CH:44]=[CH:43][C:42]=3[F:47])[N:35]=2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:2])[CH3:3]

Komponenten

6

Edukt 4

HCID 41848691-(tert-Butoxycarbonyl)-4-(methanesulfonyloxy)piperidine2×HCID 16216994BEMP resinHCID 685301764-[1-(4-chloro-phenyl)-1H-indazol-3-yloxy]-piperidine-1-carboxylic acid tert-butyl esterHCID 178518865HCID 178518865, Verbindung

Produkt 1

HCID 685328364-[4-Fluoro-1-(2-fluoro-phenyl)-1H-indazol-3-yloxy]-piperidine-1-carboxylic acid tert-butyl esterAusbeute 51 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6228DimethylformamideLösungsmittel

Versuchsvorschrift

4-[4-Fluoro-1-(2-fluoro-phenyl)-1H-indazol-3-yloxy]-piperidine-1-carboxylic acid tert-butyl ester (Intermediate 46) was prepared as described above for Intermediate 42 using Intermediate 45 (300 mg, 1.218 mmol), PS-BEMP resin (1.108 g) and 4-methanesulfonyloxy-piperidine-1-carboxylic acid tert-butyl ester (Intermediate 2) (374 mg, 1.34 mmol) in DMF (10 ml) to afford 265 mg (51%) of Intermediate 46 as a yellow oil. MS (M+1)=430.2.

Aufarbeitung

  1. custom4-[4-Fluoro-1-(2-fluoro-phenyl)-1H-indazol-3-yloxy]-piperidine-1-carboxylic acid tert-butyl ester (Intermediate 46) was prepared

Quellen und Nachweise

ORD-Eintrag
ord-150fdb8a77df4999909115a7edd9ba62
Quelldatensatz
uspto-grants-2008_09
Patentnummer
US07423054B2

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