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Route design and process development of the small nitrogen heterocycle 2·HCl, a constituent of AZD5718 (1), is described. The novel synthetic sequence to 2.HClinvolves a desymmetrizing alkylation of 4-nitropyrazole, a non-cryogenic lithiation-alkoxycarbonylation, and a global reduction-cyclization. This new synthetic route was implemented in the manufacture of 2.HCland was able to deliver over 1000 kg of product with a yield of 77% over the three stages.