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Cross-Coupling Reactions of 5-Bromo-1,2,3-triazine
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2022-10-28 , DOI: 10.1021/acs.joc.2c02082
Lukas V Hoff 1 , Joana M Hauser 1 , Karl Gademann 1
Affiliation  

An efficient Pd catalyzed cross-coupling method for 5-bromo-1,2,3-triazine is described. Optimization of the reaction conditions allowed for the preparation of a representative scope of (hetero)aryl-1,2,3-triazines (20 examples, up to 97% yield). The reaction scope was evaluated using a data science enabled boronic acid chemical space to assess the generality of the method. Additionally, diversification of the resulting products enabled the preparation of pyrimidines and pyridines in yields of up to 80% and in only two steps.

中文翻译:

5-溴-1,2,3-三嗪的交叉偶联反应

描述了 5-溴-1,2,3-三嗪的有效 Pd 催化交叉偶联方法。反应条件的优化允许制备具有代表性的(杂)芳基-1,2,3-三嗪(20 个实例,产率高达 97%)。使用支持硼酸化学空间的数据科学评估反应范围,以评估该方法的普遍性。此外,所得产品的多样化使得嘧啶和吡啶的制备收率高达 80%,并且只需两步即可完成。
更新日期:2022-10-28
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