Synthetic Route of 13544-44-0 ,Some common heterocyclic compound, 13544-44-0, molecular formula is C4HCl2IN2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
(8.1.1 ) /V-te/f-butyl^-chloro-delta-iodopyrimidin^-amine. To a solution of 2,4-dichloro-5-iodopyrimidine (10 g, 36.4 mmol) in THF (150 ml.) and DIEA (5.17 g, 6.97 ml_, 40.0 mmol) was added dropwise a solution of tert-butylamine (2.85 g, 4.09 ml_, 38.9 mmol) in THF (15 ml_). The reaction was heated to reflux and stirred over weekend at reflux temperature. The reaction mixture was cooled to room temperature, diluted with EtOAc and washed with Na2CO3-solution (2x) and brine (1x). The organic layer was dried (Na2SO4) and concentrated in vacuo to give crude product, which was purified by column chromatography (SiO2, heptane/EtOAc; 100% heptane to 20% EtOAc as mobile phase) to give the title compound in 52% yield (5.84 g, 18.7 mmol).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,13544-44-0, its application will become more common.
Reference:
Patent; N.V. ORGANON; PHARMACOPEIA, LLC; WO2009/124965; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia