55854-46-1Relevant articles and documents
2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
-
Page/Page column 217, (2021/06/26)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
New methods for the synthesis of 4H-dithieno[3,2-b:2′,3′-d]pyrrole
F?rtsch, Sebastian,Vogt, Astrid,B?uerle, Peter
, (2017/08/23)
Various alternative methods for the synthesis of 4H-dithieno[3,2-b:2′,3′-d]pyrrole (DTP) starting from commercially available bromothiophene precursors are presented. Crucial steps involve the Cadogan reaction, Ullmann-type C─N couplings, or Buchwald-Hartwig–type aminations to build up the central pyrrole ring of DTP, respectively. The use of ammonia surrogates afforded the fused target heteroacene in overall yields of 33% to 63%, and the corresponding methods are applicable on large scale.
Synthesis of Heteroaryl Sulfonamides from Organozinc Reagents and 2,4,6-Trichlorophenyl Chlorosulfate
Colombe, James R.,Debergh, J. Robb,Buchwald, Stephen L.
supporting information, p. 3170 - 3173 (2015/06/30)
A method for the preparation of aryl and heteroaryl sulfonamides using 2,4,6-trichlorophenyl chlorosulfate (TCPC) is described. The reaction of 2-pyridylzinc reagents with TCPC resulted in 2,4,6-trichlorophenyl (TCP) pyridine-2-sulfonates, and the parent pyridine-2-sulfonate was shown to react with amines. Less electron-rich aryl- and heteroarylzinc reagents reacted with TCPC to afford sulfonyl chlorides that were converted in situ to sulfonamides.