15059-17-3Relevant articles and documents
Microwave-assisted diastereoselective two-step three-component synthesis for rapid access to drug-like libraries of substituted 3-amino-β-lactams
Janssen, Guido V.,van den Heuvel, Joyce A.C.,Megens, Rik P.,Benningshof, Jorg C.J.,Ovaa, Huib
, p. 41 - 49 (2017/11/30)
Large, diverse compound libraries are an essential requisite in target-based drug development. In this work, a robust microwave-assisted synthesis for the diastereoselective generation of 3-saccharinyl-trans-β-lactams is reported. The method is optimised
Synthesis of some saccharin derivatives of expected biological activity based on n-(saccharinyl)-acetic acidazide
Arief
, p. 129 - 134 (2007/10/03)
Azide 3 was prepared from the corresponding acid chloride 2. The base catalyzed decomposition with aromatic amines, aminobenzoic acids and/or hydrazines afforded the corresponding anilides 4a-f and/or hydrazides 5a-d via azido group displacement. Compounds 5c and 5d were refluxed in Ac2O to give 1,3,4-oxadiazole derivatives 6a and 6b. Lewis acid catalyzed decomposition of azide 3 with anhyd. AlCl3 in dry aromatic substrates gave the corresponding ketones 7a-c. Also, the reaction of azide 3 with glycine gave 9.
Process for the preparation of 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides
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, (2008/06/13)
A novel process for preparing 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides is disclosed. The process involves the base catalyzed rearrangement of a saccharinacetamide of structure I to give II, STR1 wherein R1 is hydrogen or lower alkyl and R2 is lower alkyl, aryl or a heterocyclic ring selected from the group consisting of pyridyl, substituted-pyridyl, and thiazolyl. Compounds of the formula II have useful anti-inflammatory properties. In addition, they can be used as intermediate in the preparation of known anti-inflammatory agents.