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.
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.
NOVEL 2-AMINO-PYRIDINE AND 2-AMINO-PYRIMIDINE DERIVATIVES AND MEDICINAL USE THEREOF
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Paragraph 0425-0426, (2017/03/14)
Provided is a compound superior in an autotaxin inhibitory action and the like, effective as a prophylactic or therapeutic drug for diseases involving ATX. The present invention relates to a compound represented by the following formula (I): [wherein each symbol is as described in the DESCRIPTION], which has a superior autotaxin inhibitory action and is useful as a prophylactic or therapeutic drug for diseases involving ATX.