Some common heterocyclic compound, 4858-85-9, name is 2,3-Dichloropyrazine, molecular formula is C4H2Cl2N2, 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. Computed Properties of C4H2Cl2N2
A. Preparation of the intermediate compounds a) Preparation of intermediate compound 1-1 a1 ) Preparation of (1 -benzyl-piperidin-4-yl)-(3-chloro-pyrazin-2-yl)-amine; 2,3-Dichloropyrazine (10 g, 62.12 mmol) and 1 -(benzyl)-4-piperidinamine (13.73 ml_, 67.12 mmol) were dissolved in DMF (60 ml). Then Na2CO3 (10.09 g, 1 14.10 mmol) was added. The reaction was stirred at 130 0C for 16 hours. The solid was filtered off, washed with EtOAc and the solvent was evaporated till dryness. The product was dissolved in EtOAc, washed with H2O and brine, dried with MgSO4 and evaporated under vacuum. The product was used without any further purification yielding 15 g of (1 -benzyl-piperidin-4-yl)-(3-chloro-pyrazin-2-yl)-amine (74 %).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4858-85-9, its application will become more common.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; WO2008/43775; (2008); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem