The author of 《INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)》 were Yue, Eddy W.; Li, Yun-Long; Douty, Brent; He, Chunhong; Mei, Song; Wayland, Brian; Maduskuie, Thomas; Falahatpisheh, Nikoo; Sparks, Richard B.; Polam, Padmaja; Zhu, Wenyu; Glenn, Joseph; Feng, Hao; Zhang, Ke; Li, Yanlong; He, Xin; Katiyar, Kamna; Covington, Maryanne; Feldman, Patricia; Shin, Niu; Wang, Kathy He; Diamond, Sharon; Li, Yu; Koblish, Holly K.; Hall, Leslie; Scherle, Peggy; Yeleswaram, Swamy; Xue, Chu-Biao; Metcalf, Brian; Combs, Andrew P.; Yao, Wenqing. And the article was published in ACS Medicinal Chemistry Letters in 2019. Synthetic Route of C10H18INO2 The author mentioned the following in the article:
A medicinal chem. effort focused on identifying a structurally diverse candidate for phosphoinositide 3-kinase delta (PI3Kδ) led to the discovery of clin. candidate INCB050465 (20, parsaclisib). The unique structure of 20 contains a pyrazolopyrimidine hinge-binder in place of a purine motif that is present in other PI3Kδ inhibitors, such as idelalisib (1), duvelisib (2), and INCB040093 (3, dezapelisib). Parsaclisib (20) is a potent and highly selective inhibitor of PI3Kδ with drug-like ADME properties that exhibited an excellent in vivo profile as demonstrated through pharmacokinetic studies in rats, dogs, and monkeys and through pharmacodynamic and efficacy studies in a mouse Pfeiffer xenograft model. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-iodopiperidine-1-carboxylate(cas: 301673-14-3Synthetic Route of C10H18INO2)
tert-Butyl 4-iodopiperidine-1-carboxylate(cas: 301673-14-3) is one of organic iodides. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond. Iodo alkanes participate in a variety of organic synthesis reactions, which include the SimmonsSmith reaction (cyclopropanation using iodomethane), Williamson ether synthesis, Wittig reaction, Grignard reaction, alkyl coupling reactions, and Wurtz reaction.Synthetic Route of C10H18INO2
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com