501433-04-1Relevant articles and documents
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 00446, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
The basicity gradient-driven migration of iodine: Conferring regioflexibility on the substitution of fluoroarenes
Rausis, Thierry,Schlosser, Manfred
, p. 3351 - 3358 (2007/10/03)
Six different fluoroarenes were submitted to the same transformations. Direct deprotonation with alkyllithium or lithium dialkylamide as reagents and subsequent carboxylation afforded the acids 1, 6, 11, 16, 18, and 23. If the aryllithium intermediate was trapped with iodine rather than with dry ice, an iodofluoroarene (2, 7, 12, 17, 19, and 24) was formed. This, upon treatment with lithium diisopropylamide, underwent deprotonation and iodine migration. The resulting new aryllithium species was intercepted either by carboxylation, to give the acids 3, 8, 13, 20, and 25, or by neutralization, to produce the iodofluoroarenes 4, 9, 14, 21, and 26. The latter family of compounds was converted into another set of acids 5, 10, 15, 22, and 27 by subsequent treatment with butyllithium or isopropylmagnesium chloride and carbon dioxide. ( Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002).