20921-00-0Relevant articles and documents
Manufacturing Process Development for Belzutifan, Part 1: A Concise Synthesis of the Indanone Starting Material
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
, p. 508 - 515 (2021/11/24)
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.
SYNTHESIS OF TERPHENYL COMPOUNDS
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Paragraph 0066, (2017/04/11)
The present invention relates novel methods of synthesizing terphenyl compounds and in particular to novel methods for the synthesis of a compound of Formula I or intermediates thereof.
Enantioselective Synthesis of Chromenes via a Palladium-Catalyzed Asymmetric Redox-Relay Heck Reaction
Jiang, Ze-Zhen,Gao, Ang,Li, Hao,Chen, Di,Ding, Chang-Hua,Xu, Bin,Hou, Xue-Long
supporting information, p. 3119 - 3122 (2017/12/04)
A palladium-catalyzed asymmetric redox-relay Heck reaction of 4H-chromenes and arylboronic acids has been successfully developed. The reaction proceeded in moderate to good yields with good to high enantioselectivities. The resulting product is an advanced intermediate of bio-active compound BW683C.