Reference of 32111-21-0,Some common heterocyclic compound, 32111-21-0, name is 2-Iodopyrazine, molecular formula is C4H3IN2, 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.
A solution of N- (5-chloro-7-ethynyl-1, 3-benzodioxol-4-yl)-6-methoxy-7- (3- morpholin-4-ylpropoxy) quinazolin-4-amine (0.12g, 0. 24mmol), 3-iodopyrazine (O. lg, 0. 48mmol) and diisopropylamine (0. 066ml, 0. 48mmol) in ethyl acetate (3ml) was cooled to- 20 C under a nitrogen atmosphere. To this was added copper (I) iodide (0.014g, 0.072mmol) and bis (triphenylphospine) palladium (It) chloride (0.034g, 0. 048mmol). The reaction mixture was allowed to warm to ambient temperature and then stirred overnight. The mixture was filtered and the filtrate was evaporated under reduced pressure. The residue was purified by flash chromatography on silica eluting with a mixture of 0-10% methanol in dichloromethane to give the product as a light yellow solid (0.052g, 38%). NMR Spectrum: (DMSOd6) 1.99 (t, 2H), 2.40 (brs, 4H), 2.50 (t, 2H) partially obscured by DMSO peak, 3.59 (s, 4H), 3.97 (s, 3H), 4.23 (t, 2H), 6.27 (s, 2H), 7.19 (s, 1H), 7.35 (s, 1H), 7.89 (s, 1H), 8.42 (s, 1H), 8.74 (s, 1H), 8.78 (s, 1H), 8.96 (s, 1H), 9.66 (s, 1H). Mass Spectrum: M+H+ 575 and M+H-573.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Iodopyrazine, its application will become more common.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/4732; (2004); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem