Diethyl (3-aminopropyl)phosphonate → Diethyl 3-(4-(1-(2-(Dimethylamino)-6-methoxybenzyl)piperidin-4-ylamino)quinazolin-2-ylamino)propylphosphonate

HRID 215915

Reaktionsgleichung

Cl[C:2]1[N:11]=[C:10]([NH:12][CH:13]2[CH2:18][CH2:17][N:16]([CH2:19][C:20]3[C:25]([O:26][CH3:27])=[CH:24][CH:23]=[CH:22][C:21]=3[N:28]([CH3:30])[CH3:29])[CH2:15][CH2:14]2)[C:9]2[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=2)[N:3]=1.[NH2:31][CH2:32][CH2:33][CH2:34][P:35](=[O:42])([O:39][CH2:40][CH3:41])[O:36][CH2:37][CH3:38]>CCCCO>[CH3:29][N:28]([CH3:30])[C:21]1[CH:22]=[CH:23][CH:24]=[C:25]([O:26][CH3:27])[C:20]=1[CH2:19][N:16]1[CH2:17][CH2:18][CH:13]([NH:12][C:10]2[C:9]3[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=3)[N:3]=[C:2]([NH:31][CH2:32][CH2:33][CH2:34][P:35](=[O:42])([O:36][CH2:37][CH3:38])[O:39][CH2:40][CH3:41])[N:11]=2)[CH2:14][CH2:15]1

Komponenten

Reaktionsbedingungen

Temperatur: 117 °C

Versuchsvorschrift

Following General Procedure D, Compound 47 (50 mg, 0.12 mmol) and diethyl 3-aminopropylphosphonate (69 mg, 0.36 mmol) in n-BuOH (3 mL) were heated to 117° C. for 24 h with a reflux condenser. The product (Compound 81) was purified by preparative silica gel TLC plate 1000μ using 5% (7N NH3-MeOH) and 95% CH2Cl2 solution as eluent.

Aufarbeitung

customThe product (Compound 81) was purified by preparative silica gel TLC plate

Quellen und Nachweise

ORD-Eintrag: ord-ce4843057c1b49bcb9d1098f304d04c1
Quelldatensatz: uspto-grants-2012_06
DOI: 10.6084/m9.figshare.5104873.v1
Patentnummer: US08193203B2

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