- MALT1 INHIBITORS AND USES THEREOF
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The invention provides compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification which are potent inhibitors of the enzyme MALT1 and are useful in the treatment of autoimmune disorders and diseases and as an immunooncology approach to the treatment of cancer, especially bladder cancer, colon cancer, hepatocellular cancer and small cell or non-small cell lung cancer.
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Page/Page column 51-52
(2021/10/15)
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- Acid Catalyzed Chlorination of Pyrrole With N-Chloroacetanilide
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The chlorination of pyrrole with N-chloroacetanilide was catalyzed by acetic acid.Transfer of Cl+ occurred directly to the α and β positions of pyrrole and a mixture of 2-chloro-, 3-chloro- and 2,5-dichloropyrrole was formed.The α/β ratio was 10:1 under competitive conditions.
- Rosa, Michael De
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- Chlorination of Pyrrole. N-Chloropyrrole: Formation and Rearrangement to 2- and 3-Chloropyrrole
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N-Chloropyrrole (2) was formed in 65-72percent yield when pyrrole (1) in CCl4 was chlorinated with aqueous NaOCl.This intermediate rearranged in methanol to give chloropyrroles by two distinct reactions: a thermal rearrangement which gave 2-chloropyrrole (3) and an acid-catalyzed intermolecular reaction which gave 2-chloropyrrole (3), 3-chloropyrrole (4), and 2,5-dichloropyrrole (5).Nucleophilic attack on the N-Cl bond of 2 was demonstrated by reactions in the presence of CN- and SCN-.In the latter case, 2-(thiocyano)pyrrole was formed.
- Rosa, Michael De
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p. 1008 - 1010
(2007/10/02)
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