On April 19, 2019, Ku, Yi-Yin; Chan, Vincent S.; Christesen, Alan; Grieme, Timothy; Mulhern, Mathew; Pu, Yu-Ming; Wendt, Michael D. published an article.Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Development of a Convergent Large-Scale Synthesis for Venetoclax, a First-in-Class BCL-2 Selective Inhibitor. And the article contained the following:
The process development of a new synthetic route leading to an efficient and robust synthetic process for venetoclax (1: the active pharmaceutical ingredient (API) in Venclexta) is described. The redesigned synthesis features a Buchwald-Hartwig amination to construct the core ester 23c (2 tert-Bu ester) in a convergent fashion by connecting two key building blocks (4c and 26), which is then followed by a uniquely effective saponification reaction of 23c using anhydrous hydroxide generated in situ to obtain 2. Finally, the coupling of the penultimate core acid 2 with sulfonamide 3 furnishes drug substance 1 with consistently high quality. The challenges and solutions for the key Pd-catalyzed C-N cross-coupling will also be discussed in detail. The improved synthesis overcomes many of the initial scale-up challenges and was accomplished in 46% overall yield from 3,3-dimethyldicyclohexanone (6), more than doubling the overall yield of the first generation route. The new process was successfully implemented for producing large quantities of 1 with >99% area purity. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide
The Article related to venetoclax large scale synthesis buchwald hartwig amination, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics