English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

Combinatorial chemistry for the synthesis of non-peptide organic compounds has emerged as an important tool for drug discovery. 1 Solid-phase synthesis of substituted heterocyclic compounds in particular has been a focus of recent investigations with application toward a variety of drug targets. 2 As a part of our project to develop efficient synthetic methods for heterocyles, 3 we have investigated the solid-phase synthesis of 2,1,3-benzothiadiazin-4-one 2oxides as they are similar to other important heterocycles such as quinazoline-2,4-diones, 3d,4 2-thioxoquinazolin-4ones, 3a,3c 4-quinazolinones, 3b,5 1,2,4-benzothiadiazine 1,1dioxide, 1,2,4-benzothiadiazin-3-one 1,1-dioxide, 3f benzimidazole, 6 hydantoin, 7 2-piperazinone 8 Since these heterocycles have been prepared from solid-supported primary amines including nitrogen atoms as parts of the heterocyc they can easily be compared to bioactivities of 2,1,3-ben thiadiazin-4-one 2-oxides by developing the appropria solid-phase chemistry (Figure 1). Nevertheless, to the bes our knowledge, there has been only one report of the s thesis of 2,1,3-benzothiadiazin-4-one 2-oxides in solutio phase. 9 2,1,3-Benzothiadiazin-4-one 2-oxides were synth sized by reacting 2-(alkylamino)benzamides with con thionylchloride under reflux in the previous report; howeve this reaction is not suitable for our solid-phase synthesis the compounds on solid-support would be cleaved un such acidic condition. Thus, investigation was required thionylation on solid-support. In addition, preparation diverse 2-(alkylamino)benzamide was difficult with the report method; therefore, we decided to prepare 2-(alkylamin benzamides from 2-fluoro-5-nitrobenzamides through S NAr reaction. The key building block, 2-fluoro-5-nitrobenzo acid, was successfully applied to the solid-phase synthes various heterocycles, such as benzimidazoles, 10 benzopiperazinones, 11 macrocycles, 12 1,4-benzothiazepin-5-ones, 13

Efficient Solid-phase Synthesis of 2,1,3-Benzothiadiazin-4-one 2-Oxides with SynPhase™ Lanterns