2-Chloro-3-isopropoxypyrazine synthesis

Yield:-

Reaction Conditions:

at 20;

Steps:

A

To a solution of dihalide derivative (1eq.) in dry THF or dioxane or DMF was added amine (1-1.5 eq.) alone or alcohol (1-1.5 eq.) with NaH (1-5 eq.) at room temperature. After stirring for 17 hours at room temperature or 115° C., piperazine derivative (1-5 eq.) was added and the resulting mixture was heated up to 115° C. for 1 hour to 1 week. Then, the solvents were evaporated. The residue was partitioned between EtOAc and sat. NaHCO₃. The aqueous layer was extracted with EtOAc. The organic layer was washed with water, dried over MgSO₄ and concentrated to afford the crude product, which was purified by silica gel column chromatography or Shimadzu automated preparative HPLC System.

References:

US2007/249579,2007,A1 Location in patent:Page/Page column 19-20; 30