Discovery of

Some common heterocyclic compound, 40876-98-0, name is Sodium 1,4-diethoxy-1,4-dioxobut-2-en-2-olate, molecular formula is C8H11NaO5, 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. Application In Synthesis of Sodium 1,4-diethoxy-1,4-dioxobut-2-en-2-olate

Preparation of 6-hydroxy-2-phenylpyrimidine-4-carboxylic acid:; Diethyl oxaloacetate sodium salt 4.84 g (23.0 mmol) was added to a solution of 16 mL of water and 4 mL of ethanol. The suspension was stirred for 5 min, then a solution of 3.6 mL (22.5 mmol) of 6.25 M NaOH(O(? ) was added. The mixture was stirred at ambient temperature for 15 minutes to give a tan solution. To this was added a solution of 3.01 g (19.2 mmol) of benzamidine hydrochloride in 15 mL of H2O, giving a solution with pH=l 1. Next, 1 mL of 6.25 M NaOH was added, pH = 1 1 when done, then the reaction was stirred at 80 C for 2 h. Additional NaOH was added during the heating period to maintain the pH between 1 1 and 12. (A total of about 10 mmol additional NaOH was added.) The reaction was cooled to 5 C, then 12M HCl was added until pH = 1. The white precipitate was collected, washed with water, and dried on the filter to give 3.09 g (74%) of the product as a white solid.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 40876-98-0, its application will become more common.

Reference:
Patent; SIRTRIS PHARMACEUTICALS, INC.; WO2009/61453; (2009); A1;,
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