We herein report the efficient and convenient synthesis of 6-substituted-5H-pyrrolo [2, 3-b] pyrazines. The reaction is a palladium-catalyzed heteroannulation process followed by deprotection to yield the desired pyrrolo [2, 3-b] pyrazine substrates. The reaction starts with readily accessible N-(3-chloropyrazin-2-yl)-methanesulfonamide and commercially available terminal alkynes and works with aryl-and alkylalkynes.