Ethylamine → 3-(Ethylamino)-1,1,1-trifluoro-2-({[1-(4-fluorophenyl)-6-methyl-1H-indazol-4-yl]amino}methyl)-2-propanol

HRID 551433

Reaktionsgleichung

Reaktionsgleichung von HRID 551433
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[C:16]3[CH:15]=[C:14]([CH3:17])[CH:13]=[C:12]([NH:18][CH2:19][C:20]4([C:23]([F:26])([F:25])[F:24])[CH2:22][O:21]4)[C:11]=3[CH:10]=[N:9]2)=[CH:4][CH:3]=1.[CH2:27]([NH2:29])[CH3:28]>ClCCl>[CH2:27]([NH:29][CH2:22][C:20]([CH2:19][NH:18][C:12]1[CH:13]=[C:14]([CH3:17])[CH:15]=[C:16]2[C:11]=1[CH:10]=[N:9][N:8]2[C:5]1[CH:4]=[CH:3][C:2]([F:1])=[CH:7][CH:6]=1)([OH:21])[C:23]([F:25])([F:24])[F:26])[CH3:28]

Komponenten

4

Edukt 2

HCID 6341EthylamineHCID 24938054HCID 24938054, Verbindung

Produkt 1

HCID 593241453-(Ethylamino)-1,1,1-trifluoro-2-({[1-(4-fluorophenyl)-6-methyl-1H-indazol-4-yl]amino}methyl)-2-propanolAusbeute 85,7 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Versuchsvorschrift

A solution of 1-(4-fluorophenyl)-6-methyl-N-{[2-(trifluoromethyl)-2-oxiranyl]methyl}-1H-indazol-4-amine (1.52 g, 4.16 mmol) in dichloromethane (30 ml) was added to ethylamine (2M in tetrahydrofuran) (70 ml, 140 mmol). The reaction was stirred at room temperature overnight and then evaporated in vacuo. The crude product was purified on a 70 g silica Bond Elut cartridge using a 0-100% ethyl acetate in dichloromethane gradient over 60 mins to give the title compound (1.463 g).

Aufarbeitung

  1. customevaporated in vacuo
  2. customThe crude product was purified on a 70 g silica Bond Elut cartridge
  3. customover 60 mins

Quellen und Nachweise

ORD-Eintrag
ord-17c2253755db477383318d0439b5fffa
Quelldatensatz
uspto-grants-2011_05
Patentnummer
US07947727B2

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