175278-29-2Relevant articles and documents
Copper-promoted direct amidation of isoindolinone scaffolds by sodium persulfate
Lai, Huifang,Lin, Jin,Xu, Jiexin,Zha, Daijun
supporting information, p. 7621 - 7626 (2021/09/22)
Isoindolinones are ubiquitous structural motifs in natural products and pharmaceuticals. Establishing an efficient method for structural modification of isoindolinones could significantly facilitate new drug development. Herein, we describe copper-promoted direct amidation of isoindolinone scaffolds mediated by sodium persulfate. The method exhibits mild reaction conditions and high site-selectivity, and enables the structural modification of the drug indobufen ester with various amides with yields of 49 to 98%. It is also gram-scalable. Additionally, the reaction mechanism appears to involve a radical and a carbocationic pathway.
Preparation method of ovarian cancer resistance medicine Rucaparib key intermediate
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Paragraph 0024; 0030; 0031; 0035; 0036; 0040; 0041, (2018/09/11)
The invention discloses a preparation method of an ovarian cancer resistance medicine Rucaparib key intermediate, and relates to preparation of medical intermediates. A compound 1 takes methyl alcoholand cyclohexane as solvents, toluenesulfonic acid serve
Biaryl substituted hydantoin compounds as TACE inhibitors
Yu, Wensheng,Tong, Ling,Kim, Seong Heon,Wong, Michael K.C.,Chen, Lei,Yang, De-Yi,Shankar, Bandarpalle B.,Lavey, Brian J.,Zhou, Guowei,Kosinski, Aneta,Rizvi, Razia,Li, Dansu,Feltz, Robert J.,Piwinski, John J.,Rosner, Kristin E.,Shih, Neng-Yang,Siddiqui, M. Arshad,Guo, Zhuyan,Orth, Peter,Shah, Himanshu,Sun, Jing,Umland, Shelby,Lundell, Daniel J.,Niu, Xiaoda,Kozlowski, Joseph A.
scheme or table, p. 5286 - 5289 (2010/10/18)
We disclose further optimization of hydantoin TNF-α convertase enzyme (TACE) inhibitors. SAR with respect to the non-prime region of TACE active site was explored. A series of biaryl substituted hydantoin compounds was shown to have sub-nanomolar Ki