Methyl iodide → 1-Methyl-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-(nitroamino)-4(1H)-pyrimidinone

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Reaktionsgleichung

[CH3:1][N:2]1[CH:6]=[C:5]([CH2:7][C:8]2[C:9](=[O:18])[N:10]=[C:11]([NH:14][N+:15]([O-:17])=[O:16])[NH:12][CH:13]=2)[CH:4]=[N:3]1.[CH3:19]CN(C(C)C)C(C)C.CI>C(Cl)(Cl)Cl>[CH3:19][N:12]1[CH:13]=[C:8]([CH2:7][C:5]2[CH:4]=[N:3][N:2]([CH3:1])[CH:6]=2)[C:9](=[O:18])[N:10]=[C:11]1[NH:14][N+:15]([O-:17])=[O:16]

Komponenten

Reaktionsbedingungen

Temperatur: 23 °C

Versuchsvorschrift

A solution of 5-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-(nitroamino)-4(1H)-pyrimidinone (500 mg, 1.998 mmol) and DIPEA (1.745 mL, 9.99 mmol) in chloroform (5 mL) was mixed with methyl iodide (0.150 mL, 2.398 mmol). The reaction mixture was stirred at 23° C. overnight. Purification via HPLC then afforded the title compound (103 mg, 19.51% yield). LCMS: rt=1.46 min, [M+H+]=265.1

Aufarbeitung

customPurification via HPLC

Quellen und Nachweise

ORD-Eintrag: ord-02587c47211a45b9950bc505fc917ee2
Quelldatensatz: uspto-grants-2015_11
DOI: 10.6084/m9.figshare.5104873.v1
Patentnummer: US09174968B2

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