《A Continuous Flow Strategy for the Facile Synthesis and Elaboration of Semi-Saturated Heterobicyclic Fragments》 was published in European Journal of Organic Chemistry in 2019. These research results belong to Luise, Nicola; Wyatt, Eleanor W.; Tarver, Gary J.; Wyatt, Paul G.. Category: pyrazoles-derivatives The article mentions the following:
An efficient hydrogenation protocol under continuous flow conditions was developed for the synthesis of underrepresented semi-saturated bicyclic fragments containing highly sp3-rich skeletons for fragment-based drug discovery (FBDD) programs. Excellent yields were generally achieved by using Pd/C (10% weight/weight) and RaNi at 25-150° under 4-100 bar of hydrogen pressure. The generated fragments, with appropriate physicochem. properties, present diverse hydrogen-bonding pharmacophores and useful vectors for their synthetic elaboration in the optimization stage. Successive, simple functionalizations in continuous flow were accomplished to demonstrate the opportunity to develop multi-step continuous flow synthesis of valuable starting points for FBDD campaigns. A conclusive quality control (QC) was essential to discard those structures which do not fit the typical fragment library parameters. The results came from multiple reactions, including the reaction of Methyl 1H-pyrazolo[4,3-b]pyridine-6-carboxylate(cas: 1301214-72-1Category: pyrazoles-derivatives)
Methyl 1H-pyrazolo[4,3-b]pyridine-6-carboxylate(cas: 1301214-72-1) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Category: pyrazoles-derivatives
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics