4-(Chloromethyl)-1,3-thiazole hydrochloride → HCID 57974318, Verbindung

HRID 1864249Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1864249
[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]2[C:19]3[C:14](=[CH:15][CH:16]=[CH:17][C:18]=3[O:20][C@H:21]([CH3:28])[CH2:22][N:23]([CH3:27])[C:24](=[O:26])[CH3:25])[N:13]=[CH:12][N:11]=2)[CH:5]=[CH:6][C:7]=1[OH:8].Cl.Cl[CH2:31][C:32]1[N:33]=[CH:34][S:35][CH:36]=1>>[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]2[C:19]3[C:14](=[CH:15][CH:16]=[CH:17][C:18]=3[O:20][C@H:21]([CH3:28])[CH2:22][N:23]([CH3:27])[C:24](=[O:26])[CH3:25])[N:13]=[CH:12][N:11]=2)[CH:5]=[CH:6][C:7]=1[O:8][CH2:31][C:32]1[N:33]=[CH:34][S:35][CH:36]=1

Komponenten

3

Edukt 2

HCID 27632894-(Chloromethyl)-1,3-thiazole hydrochlorideHCID 69059499HCID 69059499, Verbindung

Produkt 1

HCID 57974318HCID 57974318, VerbindungAusbeute 17 %

Versuchsvorschrift

The procedure described in Example 3 was repeated using N-[(2R)-2-({4-[(3-chloro-4-hydroxyphenyl)amino]quinazolin-5-yl}oxy)propyl]-N-methylacetamide (obtained as described for in Example 50, preparation of starting materials) and 4-(chloromethyl)-thiazole hydrochloride to give the title compound in 17% yield; NMR spectrum (DMSO-d6) 1.36 (d, 3H), 1.94 (s, 3H), 3.02 (s, 3H), 3.3O (1H obscured by H2O), 4.21 (dd, 1H), 5.09 (m, 1H), 5.33 (s, 2H), 7.29 (m, 3H), 7.70 (m, 2H), 7.81 (s, 1H), 8.08 (s, 1H), 8.47 (s, 1H), 9.13 (s, 1H), 9.96 (s, 1H); Mass Spectrum MH+ 498.

Quellen und Nachweise

ORD-Eintrag
ord-3a5cdfb4d80a44fa81bde7efb52c4c7d
Quelldatensatz
uspto-grants-2009_12
Patentnummer
US07625908B2

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