Analyzing the synthesis route of 2-Chloro-5-hydroxypyrimidine

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,4983-28-2, its application will become more common.

Application of 4983-28-2, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 4983-28-2 as follows.

To a stirred solution of tert-butyl 4-hydroxypiperidine-1-carboxylate ( 2.5 g, 12.60 mmol) in THF (30 mL), 2-chloropyrimidin-5-ol (1.5 g, 11.4 mmol), TPP (7.4 g, 22.9 mmol) followed by di-tert- butyl azocarboxylate (DTAD, 5.2 g, 22.9 mmol) were added and the reaction mixture was stirred at RT overnight. Completion of the reaction was monitored by TLC. The reaction mixture was diluted with water and the aqueous layer was extracted with EtOAc (2 x 25 mL). The combined organic layer was washed with water (5 mL), brine solution (5 mL), dried over anhydrous sodium sulfate and concentrated under vacuum. The resulting crude material was purified by flash chromatography (Biotage Isolera, eluent: 50percent EtOAc in hexane) to afford the title compound. Yield: 48percent (1.8 g, yellow solid). LCMS: (Method A) 258.2 (M-f-butyl), Rt. 4.5 min, 96.8percent (Max).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,4983-28-2, its application will become more common.

Reference:
Patent; ASCENEURON S.A.; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (134 pag.)WO2019/37860; (2019); A1;,
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