2-氟-4-(反式-4-烷基环己基)苯基硼酸的合成

Synthesis of 2-Fluoro-4-(trans-4-alkylcyclohexyl)phenylboronic Acid

以1-(反式-4-烷基环己基)-3-氟苯与丁基锂、硼酸三丁酯、叔丁醇钾为反应物合成了2-氟-4-(反式-4-烷基环己基)苯基硼酸化合物3个,总收率为52%~56%,分别用IR,1HNMR对其结构进行了鉴定。优化了反应条件:n[1-(反式-4-烷基环己基)-3-氟苯]∶n(叔丁醇钾)∶n(丁基锂)∶n(硼酸三丁酯)=1∶2∶1.2∶1.5,反应温度-85^-90℃,反应时间2.5 h。叔丁醇钾的加入使反应时间由7 h缩短至2.5 h。

Three compounds of 2-fluoro-4-（trans-4-alkylcyclohexyl） phenylboronic acid were synthesized using 1-（ trans-4-alkylcyclohexyl ）-3-fluorobenzene, n-butyllithium, tributyl borate, and potassium tertbutoxide as reactants, their yields were 52% - 56%, ^1HNMR. The reaction conditions were optimized： n [ and their structures were confirmed by IR and 1-（ trans-4-alkylcyclohexyl ） -3-fluorobenzene ] ： n （ potassium tert-butoxide） ：n （ n-butyl lithium） ：n （ tributyl borate ） = 1 ： 2：1.2：1.5, reaction temperature - 85 - -90 ℃ and reaction time 2. 5 h. The addition of potassium tert-butoxide shortened the reaction time from7 h to2.5 h.