1161233-85-7Relevant articles and documents
Efficient Synthesis of Benzothiazinone Analogues with Activity against Intracellular Mycobacterium tuberculosis
Richter, Adrian,Narula, Gagandeep,Rudolph, Ines,Seidel, Rüdiger W.,Wagner, Christoph,Av-Gay, Yossef,Imming, Peter
, (2021/12/27)
8-Nitrobenzothiazinones (BTZs) are a promising class of antimycobacterial agents currently under investigation in clinical trials. Starting from thiourea derivatives, a new synthetic pathway to BTZs was established. It allows the formation of the thiazinone ring system in one synthetic step and is applicable for preparation of a wide variety of BTZ analogues. The synthetic procedure furthermore facilitates the replacement of the sulphur atom in the thiazinone ring system by oxygen or nitrogen to afford the analogous benzoxazinone and quinazolinone systems. 36 BTZ analogues were prepared and tested in luminescence-based assays for in vitro activity against Mycobacterium tuberculosis (Mtb) using the microdilution broth method and a high-throughput macrophage infection assay.
PROCESS FOR THE PREPARATION OF 2-AMINO-SUBSTITUTED 1,3-BENZOTHIAZINE-4-ONES
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Page/Page column 19, (2011/11/06)
A process for preparing 2-aminosubstituted 1, 3 -benzothiazine- 4 -ones is provided which comprises the following step: Formula (I) wherein Y is halogen; R is independently selected from C1-6-alkyl which may optionally be substituted by halogen, -NO2, halogen, -CHO -COOR4 (wherein R4 is hydrogen or C1-6-alkyl) and -CN; R3 is C1-6-alkyl which may be substituted by halogen; X is halogen; and n is 0 or an integer of 1 to 4; if n is 2, 3 or 4, multiple Rs may be the same or different.