Manufacturing Process Development for Belzutifan, Part 1: A Concise Synthesis of the Indanone Starting Material was written by Peng, Feng;Tan, Lushi;Chen, Lu;Dalby, Stephen M.;DiRocco, Daniel A.;Duan, Jianjun;Feng, Minyi;Gong, Guan;Guo, Haiheng;Hethcox, J. Caleb;Jin, Lu;Johnson, Heather C.;Kim, Jungchul;Le, Diane;Lin, Yipeng;Liu, Wenjun;Shen, Jun;Wan, Yimei;Xiao, Chengqian;Xiang, Bangping;Xiang, Qun;Xu, Jing;Yan, Luliang;Yang, Weiyi;Ye, Honglin;Yu, Yanpei;Zhang, Jun. And the article was included in Organic Process Research & Development in 2022.Electric Literature of C4H4BrNO2 This article mentions the following:
A four-step synthesis of the indanone core of belzutifan (MK-6482) is described. This route starts from the commodity raw material dihydrocoumarin and was successfully demonstrated on a large scale to produce indanone 11 in the synthesis of belzutifan, an FDA-approved first-in-class therapy for the treatment of patients with certain types of Von Hippel-Lindau disease-associated tumors. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Electric Literature of C4H4BrNO2).
1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Electric Literature of C4H4BrNO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary