1H-1,2,4-Triazole → Anastrozole

HRID 1669818Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1669818
[C:1]([C:3]([C:6]1[CH:7]=[C:8]([CH:11]=[C:12]([C:14]([C:17]#[N:18])([CH3:16])[CH3:15])[CH:13]=1)[CH2:9]Br)([CH3:5])[CH3:4])#[N:2].[NH:19]1[CH:23]=[N:22][CH:21]=[N:20]1>[Br-].C([N+](CCCC)(CCCC)CCCC)CCC>[CH3:4][C:3]([C:6]1[CH:7]=[C:8]([CH2:9][N:19]2[N:20]=[CH:21][N:22]=[CH:23]2)[CH:11]=[C:12]([C:14]([C:17]#[N:18])([CH3:16])[CH3:15])[CH:13]=1)([C:1]#[N:2])[CH3:5]

Komponenten

4

Edukt 2

HCID 92571H-1,2,4-TriazoleHCID 115223592,2'-(5-Bromomethyl-1,3-phenylene)di(2-methylpropiononitrile)

Produkt 1

HCID 2187Anastrozole

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 74236Tetrabutylammonium BromideKatalysator

Versuchsvorschrift

In yet another embodiment of the present invention, the purified bromo compound (formula (III)) is alkylated with 1,2,4-triazole in a suitable solvent using a suitable base in the presence of a phase transfer catalyst such as tetrabutyl ammonium bromide to obtain anastrozole, which is further purified using column chromatography, followed by precipitation/crystallization using ethyl acetate and diisopropyl ether to obtain pure anastrozole in high yield.

Quellen und Nachweise

ORD-Eintrag
ord-f88e4f2f632742f4a2220759f70d17bc
Quelldatensatz
uspto-grants-2011_08
Patentnummer
US07989636B2

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