[1-(Methylsulfonyl)piperidin-4-yl]amine trifluoroacetate → [2-Amino-6-(1-methanesulfonyl-piperidin-4-ylamino)-pyridin-3-yl]-(4-chloro-5-fluoro-2-methoxy-phenyl)-methanone

HRID 30146

Reaktionsgleichung

Reaktionsgleichung von HRID 30146
[NH2:1][C:2]1[C:7]([C:8]([C:10]2[CH:15]=[C:14]([F:16])[C:13]([Cl:17])=[CH:12][C:11]=2[O:18][CH3:19])=[O:9])=[CH:6][CH:5]=[C:4](Cl)[N:3]=1.FC(F)(F)C(O)=O.[CH3:28][S:29]([N:32]1[CH2:37][CH2:36][CH:35]([NH2:38])[CH2:34][CH2:33]1)(=[O:31])=[O:30]>>[NH2:1][C:2]1[C:7]([C:8]([C:10]2[CH:15]=[C:14]([F:16])[C:13]([Cl:17])=[CH:12][C:11]=2[O:18][CH3:19])=[O:9])=[CH:6][CH:5]=[C:4]([NH:38][CH:35]2[CH2:36][CH2:37][N:32]([S:29]([CH3:28])(=[O:31])=[O:30])[CH2:33][CH2:34]2)[N:3]=1

Komponenten

3

Edukt 2

HCID 11975076[1-(Methylsulfonyl)piperidin-4-yl]amine trifluoroacetateHCID 58590823(2-Amino-6-chloro-pyridin-3-yl)-(4-chloro-5-fluoro-2-methoxy-phenyl)-methanone

Produkt 1

HCID 11705192[2-Amino-6-(1-methanesulfonyl-piperidin-4-ylamino)-pyridin-3-yl]-(4-chloro-5-fluoro-2-methoxy-phenyl)-methanone

Versuchsvorschrift

The title compound was prepared from (2-Amino-6-chloro-pyridin-3-yl)-(4-chloro-5-fluoro-2-methoxy-phenyl)-methanone (Example 47) and 1-methanesulfonyl-piperidin-4-ylamine (Step A, Example 6) using the procedure described in Step B. Example 6. HRMS, observed: 457.1106, Calcd for (M+H)+: 457.1107. Ki for cdk4=0.008 μM, cdk1=0.154 μM, cdk2=0.039 μM, and IC50 for HCT116 cell line=3.0 μM.

Quellen und Nachweise

ORD-Eintrag
ord-8be0577ea87f4689af3358b7a02cb424
Quelldatensatz
uspto-grants-2008_09
Patentnummer
US07423051B2

Verknüpfte Notizen

Wird geladen…