Triethylamine → 2-(3-Fluoro-phenyl)-5-[4-(5-methyl-isoxazol-4-ylmethyl)-piperazin-1-yl]-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-ylamine

HRID 1181298Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1181298
Cl[CH2:2][C:3]1[CH:4]=[N:5][O:6][C:7]=1[CH3:8].[F:9][C:10]1[CH:11]=[C:12]([C:16]2[N:31]=[C:19]3[N:20]=[C:21]([N:25]4[CH2:30][CH2:29][NH:28][CH2:27][CH2:26]4)[N:22]=[C:23]([NH2:24])[N:18]3[N:17]=2)[CH:13]=[CH:14][CH:15]=1.CCN(CC)CC>CC#N>[F:9][C:10]1[CH:11]=[C:12]([C:16]2[N:31]=[C:19]3[N:20]=[C:21]([N:25]4[CH2:26][CH2:27][N:28]([CH2:2][C:3]5[CH:4]=[N:5][O:6][C:7]=5[CH3:8])[CH2:29][CH2:30]4)[N:22]=[C:23]([NH2:24])[N:18]3[N:17]=2)[CH:13]=[CH:14][CH:15]=1

Komponenten

5

Edukt 3

HCID 8471TriethylamineHCID 138497564-(Chloromethyl)-5-methyl-1,2-oxazoleHCID 694310402-(3-Fluoro-phenyl)-5-piperazin-1-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-ylamine

Produkt 1

HCID 114866512-(3-Fluoro-phenyl)-5-[4-(5-methyl-isoxazol-4-ylmethyl)-piperazin-1-yl]-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-ylamine

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6342AcetonitrileLösungsmittel

Versuchsvorschrift

4-Chloromethyl-5-methyl-isoxazole (1.5 eq.) was directly added to a solution of 2-(3-fluoro-phenyl)-5-piperazin-1-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-ylamine (0.14 mmol; see Example 10(a) above) and Et3N (0.3 mmol) in 3 mL of CH3CN. The resulting reaction mixture was stirred at room temp for 18 hours. It was then concentrated and purified by preparative HPLC using a mixture of aqueous CH3CN that has been buffered with 0.1% TFA.

Aufarbeitung

  1. customThe resulting reaction mixture
  2. concentrationIt was then concentrated
  3. custompurified by preparative HPLC
  4. additiona mixture of aqueous CH3CN that

Quellen und Nachweise

ORD-Eintrag
ord-4bababde052d4b24a9d58085e6d2f4a5
Quelldatensatz
uspto-grants-2007_10
Patentnummer
US07285550B2

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