Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.
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Paragraph 00629
(2020/03/02)
A procedure for transforming indoles into indolequinones
A procedure that converts a series of structurally diverse, readily available indole derivatives to their corresponding indolequinones is described. The three-step route commences with an iridium catalyzed C-H borylation to give a 7-borylindole that upon
Eastabrook, Andrew S.,Wang, Christy,Davison, Emma K.,Sperry, Jonathan
p. 1006 - 1017
(2015/01/30)
A highly selective Ir-catalyzed borylation of 2-substituted indoles: a new access to 2,7- and 2,4,7-substituted indoles
The selective CH-functionalization of 2-substituted indoles is presented. Using bis(pinacolato)diboron (2) in the presence of iridium complexes, a novel catalytic mono-borylation is observed preferentially at the 7-position of the indole. This allows for
Lo, Wei Fun,Kaiser, Hanns Martin,Spannenberg, Anke,Beller, Matthias,Tse, Man Kin
p. 371 - 375
(2007/10/03)
Ir-catalyzed functionalization of 2-substituted indoles at the 7-position: Nitrogen-directed aromatic borylation
Ir-catalyzed borylation of 2-substituted indoles selectively yields 7-borylated products in good yields. N-Protection, required for previous functionalizations of 2-substituted indoles, is unnecessary. Copyright
Paul, Sulagna,Chotana, Ghayoor A.,Holmes, Daniel,Reichle, Rebecca C.,Maleczka Jr., Robert E.,Smith III, Milton R.
p. 15552 - 15553
(2007/10/03)
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