A new synthetic route of 60154-05-4

Statistics shows that 60154-05-4 is playing an increasingly important role. we look forward to future research findings about 5-Iodo-1-methylpyridin-2(1H)-one.

Electric Literature of 60154-05-4, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.60154-05-4, name is 5-Iodo-1-methylpyridin-2(1H)-one, molecular formula is C6H6INO, molecular weight is 235.0224, as common compound, the synthetic route is as follows.

5 -((tert-butyldimethylsilyl)oxy)-6-chloro- 1H-indazole (0.70 g) and 5 -iodo- 1-methylpyridin-2(1H)-one (Example 1, Step B) (0.64 g, 2.7 mmol) were mixed in toluene(2 mL) and heated gently to dissolve at 50C. The resulting mixture was evacuated andpurged with N2 several times. Potassium phosphate (0.43 mL, 5.2 mmol) and (1S,2S)-cyclohexane-1,2-diamine (0.060 mL, 0.50 mmol) were added, followed by copper(I) iodide (0.028 g, 0.15 mmol). The mixture was then heated to 110C for 19 hr. Afterward, the mixture was cooled to room temperature and diluted with ethyl acetate (120 mL), washed with 1M HC1 (50 mL), and saturated ascorbic acid (30 mL). The organic andaqueous layers were separated on a phase separator. The organic layer was concentrated to yield 1.2 g of the title product as a purple/brown oil that was used in the next step without further purification.

Statistics shows that 60154-05-4 is playing an increasingly important role. we look forward to future research findings about 5-Iodo-1-methylpyridin-2(1H)-one.

Reference:
Patent; ASTRAZENECA; RIPA, Lena, Elisabeth; LAWITZ, Karolina; LEPISTOe, Matti, Juhani; HEMMERLING, Martin; EDMAN, Karl; LLINAS, Antonio; (96 pag.)WO2016/46260; (2016); A1;,
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