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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 415395Generated: October 25, 2026

Diisopropylethylamine → Azd-1480

https://huagongshe.com/reaction/415395

Reaction equation

Participants

RoleNameHCIDCharge
ReactantDiisopropylethylamineHCID 81531—
Reactant2,5-Dichloro-N-(5-methyl-1H-pyrazol-3-yl)-4-pyrimidinamineHCID 11402272—
Reactant(S)-1-(5-Fluoropyrimidin-2-yl)ethanamine hydrochlorideHCID 66624037—
Solvent1-ButanolHCID 263—
ProductAzd-1480HCID 1665984157.3%

Reaction Conditions

Temperature180 °C

Reaction Steps

A mixture of (5)-1-(5-fluoropyrimidin-2-yl)ethanamine hydrochloride (Method 7, 80 mg), 2,5-dichloro-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine (Method 9, 122 mg) and DIPEA (0.134 ml) in n-BuOH (2.5 ml) was charged into a microwave reaction vessel. The vessel was sealed and heated in microwave reactor at 180° C. for 6 hours. The solvent was removed under reduced pressure and the residue was purified by Gilson (10-50% MeCN/H2O, 15 min) to give the titled compound as solid (90 mg). NMR 10.34 (s, 1H), 8.91 (s, 3H), 8.30 (s, 1H), 5.94 (s, 1H), 4.96-5.34 (m, 1H), 2.25 (s, 3H), 1.56 (d, 3H); m/z 350.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08088784B2
Source datasetuspto-grants-2012_01
ORD IDord-fd2a37867f3f4dda9343db6628b04a5f
Source noteuspto-grants-2012_01