26673-31-4Relevant articles and documents
PROCESSES AND INTERMEDIATES FOR PREPARING MCL1 INHIBITORS
-
Paragraph 0190, (2021/06/04)
The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
The Electrophilic Fluorination of Enol Esters Using SelectFluor: A Polar Two-Electron Process
Wood, Susanna H.,Etridge, Stephen,Kennedy, Alan R.,Percy, Jonathan M.,Nelson, David J.
supporting information, p. 5574 - 5585 (2019/03/21)
The reaction of enol esters with SelectFluor is facile and leads to the corresponding α-fluoroketones under mild conditions and, as a result, this route is commonly employed for the synthesis of medicinally important compounds such as fluorinated steroids. However, despite the use of this methodology in synthesis, the mechanism of this reaction and the influence of structure on reactivity are unclear. A rigorous mechanistic study of the fluorination of these substrates is presented, informed primarily by detailed and robust kinetic experiments. The results of this study implicate a polar two-electron process via an oxygen-stabilised carbenium species, rather than a single-electron process involving radical intermediates. The structure–reactivity relationships revealed here will assist synthetic chemists in deploying this type of methodology in the syntheses of α-fluoroketones.
Acid-promoted furan annulation and aromatization: An access to benzo[b]furan derivatives
Ao, Jun,Liu, Yidong,Jia, Shiqi,Xue, Lu,Li, Dongmei,Tan, Yu,Qin, Wenling,Yan, Hailong
supporting information, p. 433 - 440 (2018/01/03)
An unprecedented PTSA-promoted furan annulation and aromatization in one pot has been developed. This process offers a simple and efficient synthetic route for the construction of various highly substituted benzo[b]furan derivatives, which are widely used not only in drug active molecules but also organic semiconductor and organic light-emitting devices. The preliminary mechanism study indicated this transformation proceeded sequentially via furan annulation and aromatization.