An optimized cost-effective synthesis of the new antitussive drug, DF1012 (I), is reported.The new synthetic route to the key intermediate, 7-azaindolyl-3-carboxylic acid, is based on the unusual deprotection step of the 1-tert-butyl-3-cyano-7-azaindole and can also be regarded as a convenient way for the industrial production of the expensive unsubstituted 7-azaindole.The second key intermediate, endo-tropanamine, was obtained in high yield by a novel one-pot stereoselective process using a Pd-catalyzed reductive amination procedure.