73998-95-5Relevant articles and documents
Development of a Rapid Scale-Up Synthesis of (S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide, a Potent Adaptor-Associated Kinase 1 Inhibitor
Li, Jianqing,Smith, Daniel,Pawluczyk, Joseph,Krishnananthan, Subramaniam,Wang, Bei,Hou, Xiaoping,Zhao, Rulin,Kempson, James,Sun, Dawn,Yip, Shiuhang,Wu, Dauh-Rurng,Maddala, Nageswararao,Vetrichelvan, Muthalagu,Gupta, Anuradha,Macor, John E.,Dzierba, Carolyn D.,Mathur, Arvind
supporting information, p. 437 - 446 (2022/02/09)
(S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide (1) is a potent adaptor-associated kinase 1 inhibitor, which may have the potential to treat neuropathic pain and other neurological disorders including schizophrenia, Parkinson’s disease, bipolar disorder, and Alzheimer’s disease. For preclinical studies, a substantial amount of high-quality material was required. The original discovery route for the preparation of this compound suffered from scale-up issues that included a very low-yielding C-O coupling step and the use of expensive and toxic reagents. This paper describes a rapid scale-up synthesis accomplished in eight steps, which involves the coupling of phenol 17 with oxathiazolidine 18 as the key transformation.
CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS
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Paragraph 00289, (2019/02/25)
The present disclosure relates to modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors, and methods of using the inhibitors. The modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25 can be useful in the treatment of cancers, among other ailments.
3,4-dihydropyrido[4,3-d]pyrimidine derivative, and preparation method and use thereof
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Paragraph 0069; 0072; 0083-0085, (2019/10/07)
The invention relates to a 3,4-dihydropyrido[4,3-d]pyrimidine derivative, and a preparation method and a use thereof. The compound is a compound represented by formula I, or a pharmaceutically acceptable salt or stereoisomer or tautomer thereof, and R to R are as defined in the description.