Some tips on 4,6-Dichloropyrimidine-5-carbaldehyde

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,5305-40-8, its application will become more common.

Reference of 5305-40-8 ,Some common heterocyclic compound, 5305-40-8, molecular formula is C5H2Cl2N2O, 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.

Hydrazine hydrate (2.0 ml, 41 mmol) was slowly added to a solution of 4,6- dichloropyrimidine-5-carbaldehyde (7.2 g, 41 mmol) in MeOH (150 ml) -60 0C (nitromethane-dry ice bath) followed by triethylamine (6.8 mL, 49 mmol). The mixture was allowed to warm to rt and stirred for 2 h. MeOH was removed in vacuo and water (150 mL) was added. The mixture was extracted with EtOAc (3 x 80 mL). The combined organic layers were washed with brine (100 mL), dried over Na2SO4, and filtered through a glass funnel. Removal of solvent gave 4-chloro-lH-pyrazolo[3,4-d]pyrimidine (4.45 g, 71%). MS (ESI, pos. ion) m/z: 155 [M+H]+

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,5305-40-8, its application will become more common.

Reference:
Patent; AMGEN INC.; WO2008/153947; (2008); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia