690636-28-3Relevant articles and documents
Synthesis method of tirbanibulin intermediate
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Paragraph 0028-0033; 0036-0042, (2022/01/10)
The invention belongs to the technical field of synthesis of medical compounds, and particularly discloses a synthesis method of a tirbanibulin intermediate. According to the method, 4-[2-(4-bromophenoxy)ethyl]morpholine is adopted as a raw material, firstly reacts with an n-butyl magnesium lithium reagent and then reacts with isopropyl alcohol pinacol borate, and the tirbanibulin intermediate is synthesized through a one-pot method. The method is mild in reaction condition and simple to operate, the reaction product is single, the target product can be obtained at high yield through a simple post-treatment and recrystallization method, and the method is expected to be developed into an industrial production method.
IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS
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Paragraph 00110, (2020/06/05)
The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH.
In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors
Tasker, Nikhil R.,Rastelli, Ettore J.,Blanco, Isabella K.,Burnett, James C.,Sharlow, Elizabeth R.,Lazo, John S.,Wipf, Peter
supporting information, p. 2448 - 2466 (2019/03/06)
A continuous flow photooxygenation of 7-aminothieno[3,2-c]pyridin-4(5H)-ones to produce 7-iminothieno[3,2-c]pyridine-4,6(5H,7H)-diones has been developed, utilizing ambient air as the sole reactant. N-H Imines are formed as the major products, and excellent functional group tolerance and conversion on gram-scale without the need for chromatographic purification allow for facile late-stage diversification of the aminothienopyridinone scaffold. Several analogs exhibit potent in vitro inhibition of the cancer-associated protein tyrosine phosphatase PTP4A3, and the SAR supports an exploratory docking model.