https://doi.org/10.1071/CH18045
Serena Monticelli
A and Vittorio PaceA,B
ADepartment of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, A-1090
Vienna, Austria.
B
Manuscript received: 29 January 2018.
Manuscript accepted: 11 April 2018.
Published online: 7 May 2018.Vittorio Pace received his Ph.D. in Chemical Sciences from the Complutense University of Madrid in 2010. After post-doctoral training at Vienna, Manchester, and Stockholm, he
obtained a tenure track position at the University of Vienna. In 2016 he received the Habilitation in Pharmaceutical Chemistry from the University of Vienna and in 2017 the
Habilitation for Full Professor of Organic Chemistry
背景
氟代碘甲烷(氟瑞医药可提供)(FCH2I,CAS 373-53-5)是易溶于液体的液体(bp 53.48C)
可以用作氟甲基(CH2F)单元的前体。 C1大嵌段对两个碳卤素键的反应性不同:因此,CH2-1连接可以方便地用于完成亲核取代,
[1]
碘-金属交换或过渡金属催化的过程,留下氟完整的omethyl基序。芳环的氟甲基化2015年,胡报告了第一个直接钯催化的直接具有ICH2F作为氟甲基供体的芳基硼酸酯的单氟甲基化单位(方案1)。
[2]
由于温和的反应条件和非常好的官能团耐受性,该方案特别有吸引力。 从这个意义上说,胡的程序改进了铃木以前的工作,其中涉及氟化苄的制备使用频哪醇硼酸酯(40当量)和化学计量的钯。[3]
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