- Alluzole intermediate and method for preparing
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The invention relates to an intermediate and a preparation method thereof, and adopts a compound as shown in a formula (4). For the preparation of, 4 is R in the formula (- COOR). 1 Or CONH2 , R1 Alkyl or aryl. The compound represented by the formula (4) is represented by the formula (3). Reaction of acyl chloride with acylating agent The acid chloride is then reacted with the thiocyanide to form. To the application, a new material formula (4) is used as an intermediate to synthesize the, and a brand new process route for synthesizing the is developed, and the process route is good in stability and good in repeatability, and is very suitable for industrial production.
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Paragraph 0093-0097
(2021/09/21)
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- Method for preparing
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The invention relates to a method for preparing an intermediate and an epalutamide, wherein the compound is represented by the formula (5). The preparation method of the compound represented by the formula (5) comprises the following steps: preparing compound represented by formula (3) by using the compound as an intermediate. Compound of formula (4) and Thithio reagent is reacted to form the compound represented by formula (5). The thio reagent is a phenyl thioformate. A combination of one or more N-thiocarbonyldiimidazole, 1,1 -thiocarbonyl DI-2 (1H) - pyridine. The inventors have found that 4 - (1 - carboxamide - cyclobutylamino) -2 - fluoro - N - methyl - benzamide, 5 - amino -2 - cyano -3 - trifluoromethyl pyridine and sodium thiochloroformate can be obtained in a higher yield than the prior art by one-step reaction under appropriate conditions. Based on this finding, the present invention was obtained and presented by further study.
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