Automated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis was written by Liu, Chenguang;Xie, Jiaxun;Wu, Wenbin;Wang, Mu;Chen, Weihao;Idres, Shabana Binte;Rong, Jiawei;Deng, Lih-Wen;Khan, Saif A.;Wu, Jie. And the article was included in Nature Chemistry in 2021.Related Products of 700-16-3 The following contents are mentioned in the article:
Recent advances in end-to-end continuous-flow synthesis are rapidly expanding the capabilities of automated customized syntheses of small-mol. pharmacophores, resulting in considerable industrial and societal impacts; however, many hurdles persist that limit the number of sequential steps that can be achieved in such systems, including solvent and reagent incompatibility between individual steps, cumulated byproduct formation, risk of clogging and mismatch of timescales between steps in a processing chain. To address these limitations, herein a strategy that merges solid-phase synthesis and continuous-flow operation, enabling push-button automated multistep syntheses of active pharmaceutical ingredients, is reported. The application of this methodol. is demonstrated with a six-step synthesis of prexasertib in 65% isolated yield after 32 h of continuous execution. As there are no interactions between individual synthetic steps in the sequence, the established chem. recipe file was directly adopted or slightly modified for the synthesis of twenty-three prexasertib derivatives, enabling both automated early and late-stage diversification. This study involved multiple reactions and reactants, such as 2,3,4,5,6-Perfluoropyridine (cas: 700-16-3Related Products of 700-16-3).
2,3,4,5,6-Perfluoropyridine (cas: 700-16-3) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Related Products of 700-16-3