2613-38-9Relevant articles and documents
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
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Page/Page column 143-144, (2020/11/23)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is -NHSO2- or -SO2NH-; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one ormore substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl,Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl andhaloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl,SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionallysubstituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno- oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
Transition-metal-free synthesis of phenanthridinones from biaryl-2-oxamic acid under radical conditions
Yuan, Ming,Chen, Li,Wang, Junwei,Chen, Shenjie,Wang, Kongchao,Xue, Yongbo,Yao, Guangmin,Luo, Zengwei,Zhang, Yonghui
supporting information, p. 346 - 349 (2015/02/19)
Na2S2O8-promoted decarboxylative cyclization of biaryl-2-oxamic acid for phenanthridinones has been developed. This work illustrates the first example of intramolecular decarboxylative amidation of unactivated arene under transition-metal-free conditions. Additionally, this approach provides an efficient and economical method to access biologically interesting phenanthridinones, an important structure motif in many natural products. (Chemical Equation Presented).
An easily prepared tetraphosphine and its use in the palladium-catalyzed Suzuki-Miyaura coupling of aryl chlorides
Wang, Kun,Wang, Wei,Luo, Heng,Zheng, Xueli,Fu, Haiyan,Chen, Hua,Li, Ruixiang
, p. 1214 - 1219 (2014/01/06)
An air-stable tetraphosphine N,N,N′,N′- tetra(diphenylphosphinomethyl)-benzene-1,3-diamine (L3) was easily prepared in two steps from triphenylphosphine, which in combination with [Pd(η3-C3H5)Cl]2 affords an efficient catalyst for Suzuki-Miyaura coupling of activated chloroarenes. Even at high temperature of 130 C, this catalyst exhibits good stability and longevity, and could allow a high turnover number of 680,000 to be reached. Graphical Abstract: [Figure not available: see fulltext.].