- RECYCLIZATION OF PYRROLOPYRAZINIUM SALTS INTO 6- AND 8-AMINOINDOLIZINES
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Recyclization of 3-alkylpyrrolopyrazinium salts in the presence of base afforded derivatives of 6-aminoindolizine.Rearrangement of 1,3-dialkylpyrrolopyrazinium salts proceeded in two directions, giving rise to both 6- and 8-aminoindolizines,
- Terenin, V. I.,Kabanova, E. V.,Feoktistova, E. S.,Bundel', Yu. G.
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- EIS INHIBITORS
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Compounds and compositions are disclosed, which are useful as inhibitors of acetyltransferase Eis, a mediator of kanamycin resistance in Mycobacterium tuberculosis.
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Paragraph 0025; 0131; 0132; 0133
(2018/06/30)
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- Combating Enhanced Intracellular Survival (Eis)-Mediated Kanamycin Resistance of Mycobacterium tuberculosis by Novel Pyrrolo[1,5-a]pyrazine-Based Eis Inhibitors
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Tuberculosis (TB) remains one of the leading causes of mortality worldwide. Hence, the identification of highly effective antitubercular drugs with novel modes of action is crucial. In this paper, we report the discovery and development of pyrrolo[1,5-a]p
- Garzan, Atefeh,Willby, Melisa J.,Ngo, Huy X.,Gajadeera, Chathurada S.,Green, Keith D.,Holbrook, Selina Y. L.,Hou, Caixia,Posey, James E.,Tsodikov, Oleg V.,Garneau-Tsodikova, Sylvie
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p. 302 - 309
(2017/04/21)
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- Pyrrolodiazines. 6. Palladium-catalyzed arylation, heteroarylation, and amination of 3,4-dihydropyrrolo[1,2-α]pyrazines
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The palladium-catalyzed Suzuki cross-coupling reaction of arylboronic acids and 6-bromo- and 6,8-dibromo-3,4-dihydropyrrolo[1,2-α]pyrazines afforded 6-substituted and 6,8-disubstituted 3,4-dihydropyrrolo[1,2-α]pyrazines in good yields. Stille and Negishi coupling reactions have been used to prepare 6-heteroaryl-substituted derivatives in moderate yields by employing heteroaryl halides and 6-metalated 3,4-dihydropyrrolo[1,2-α]pyrazines as reaction partners. A variety of cyclic secondary amines have also been incorporated at position C-6 of 6-bromo-1-phenyl-3,4-dihydropyrrolo[1,2-α]pyrazine in the presence of the palladium catalyst Pd2(dba)3 in conjunction with BINAP as ligand. This amination reaction is one of the few reported examples of such a palladium-catalyzed transformation on a pyrrole ring, although the reaction could not be extended to less nucleophilic amines.
- Castellote, Isabel,Vaquero, Juan J.,Fernandez-Gadea, Javier,Alvarez-Builla, Julio
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p. 8668 - 8675
(2007/10/03)
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- AZACYCLOALKANES. XXIX. SYNTHESIS OF 1-SUBSTITUTED 3,4-DIHYDROPYRROLOPYRAZINES
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The reaction of 2-acylfurans with ethylenediamine is a general method for the production of 1-substituted 3,4-dihydropyrrolopyrazines.
- Likhosherstov, A. M.,Peresada, V. P.,Vinokurov, V. G.,Skoldinov, A. P.
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p. 2341 - 2345
(2007/10/02)
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