Analysis and purification of boronic acid pinacol esters by RPLC is very challenging due to their degradation in aqueous and alcoholic solvents. These compounds are difficult to purify by SFC too as they are equally sensitive to traditional co-solvents like methanol, ethanol, and 2-propanol. 2,2,2 trifluoroethanol (TFE), which has been reported for the purification of a few alcohol sensitive compounds, was evaluated as a co-solvent in this study for the purification of chiral and achiral boronate esters by SFC. Examples of twelve compounds were presented in this paper where degradation of boronic acid pinacol esters was successfully controlled by replacing methanol with TFE as the co-solvent in SFC. A separate study showed that TFE can also control the epimerization of the enantiomers of 3 substituted 1,4 benzodiazepine analogues during the purification process. In addition to above benefits, 2,2,2trifloroethanol showed improved selectivity and resolution for most of the compounds. With its stronger solvent strength compared to other alcohols, TFE could also be used to reduce the co-solvent percentage needed for elution and to shorten retention time of highly polar samples which did not elute even in 50% of other co-solvents in SFC. A case study of compound B demonstrated that TFE provided a reduced co-solvent percentage and a shorter cycle time with much improved resolution as compared to methanol, thus resulting in higher loading and throughput with reduction of total solvent consumption.

通过RPLC分析和纯化硼酸频哪醇酯是非常具有挑战性的，因为它们在水性和醇性溶剂中会降解。这些化合物也难以通过SFC纯化，因为它们对传统的助溶剂（如甲醇，乙醇和2-丙醇）同样敏感。2,2,2三氟乙醇（TFE），已报道用于纯化一些对酒精敏感的化合物，在本研究中被评估为助溶剂，用于通过SFC纯化手性和非手性硼酸酯。本文介绍了十二种化合物的实例，其中通过用TFE代替甲醇作为SFC中的助溶剂，成功控制了硼酸频哪醇酯的降解。另一项研究表明，TFE还可以控制3个取代的1对映体的差向异构 在纯化过程中有4种苯并二氮杂analogue类似物。除上述优点外，2,2,2-三氟乙醇对大多数化合物显示出更高的选择性和分离度。与其他醇相比，TFE具有更强的溶剂强度，因此还可用于降低洗脱所需的助溶剂百分比，并缩短即使在50％的SFC中也无法洗脱的高极性样品的保留时间。化合物B的一项案例研究表明，与甲醇相比，TFE提供了降低的助溶剂百分比和更短的循环时间，且分离度大大提高，从而提高了载量和通量，同时减少了总溶剂消耗。与其他醇相比，TFE具有更强的溶剂强度，因此还可用于降低洗脱所需的助溶剂百分比，并缩短即使在50％的SFC中也无法洗脱的高极性样品的保留时间。化合物B的一项案例研究表明，与甲醇相比，TFE提供了降低的助溶剂百分比和更短的循环时间，且分离度大大提高，从而提高了载量和通量，同时减少了总溶剂消耗。与其他醇相比，TFE具有更强的溶剂强度，因此还可用于降低洗脱所需的助溶剂百分比，并缩短即使在50％的SFC中也无法洗脱的高极性样品的保留时间。化合物B的案例研究表明，与甲醇相比，TFE提供了降低的助溶剂百分比和更短的循环时间，且分离度大大提高，从而导致了更高的负载量和通量，同时减少了总溶剂消耗。