15246-95-4

Upstream product

• 128-44-9 saccharin sodium salt 
• 70-11-1 α-bromoacetophenone 
• 182925-82-2 N-(saccharinyl)-acetic acid azide 
• 71-43-2 benzene 
• 98-86-2 acetophenone 
• 81-07-2 saccharin 
• 13735-81-4 1-styrenyloxytrimethylsilane 
• 61020-33-5 2-[1,1-dioxide-3-oxo-1,2-benzisothiazole-2(3H)-yl] acetic acid chloride 
• 52188-11-1 2-(1,1-dioxido-3-oxobenzo[d]isothiazol-2(3H)-yl)acetic acid 

Downstream Products

• 3278-14-6 N-phenethylbenzamide 
• 128328-80-3 2-(1-Benzoyl-2,2-bis-benzylsulfanyl-vinyl)-1,1-dioxo-1,2-dihydro-1λ⁶-benzo[d]isothiazol-3-one 
• 128328-79-0 2-(1-Benzoyl-2,2-bis-ethylsulfanyl-vinyl)-1,1-dioxo-1,2-dihydro-1λ⁶-benzo[d]isothiazol-3-one 
• 128328-78-9 2-(1-Benzoyl-2,2-bis-methylsulfanyl-vinyl)-1,1-dioxo-1,2-dihydro-1λ⁶-benzo[d]isothiazol-3-one 
• 101097-95-4 2-phenacylsulfamoyl-benzoic acid 
• 903865-07-6 methyl [4-hydroxy-1,1-dioxido-3-(phenylcarbonyl)-2H-1,2-benzothiazin-2-yl]acetate 
• 1447945-17-6 2-(5,5-dioxido-3-phenylpyrazolo[4,3-c][1,2]benzothiazin-4(2H)-yl)acetohydrazide 
• 1421740-44-4 4-methyl-3-phenyl-2,4-dihydrobenzo[e]pyrazolo[4,3-c][1,2]thiazine 5,5-dioxide 

Relevant academic research and scientific papers

Synthesis and pharmacological evaluation of novel arylpiperazine oxicams derivatives as potent analgesics without ulcerogenicity

Gastrotoxicity continues to be a major issue in therapy with nonsteroidal anti-inflammatory drugs (NSAIDs). Medicine is yet to develop absolutely safe analgesics. Numerous strategies are employed to discover new, safer NSAIDs, for example selective inhibi

Stereopure Functionalized Benzosultams via Ruthenium(II)-Catalyzed Dynamic Kinetic Resolution-Asymmetric Transfer Hydrogenation

A highly diastereo- and enantioselective Ru(II)-catalyzed dynamic kinetic resolution-asymmetric transfer hydrogenation (DKR-ATH) of α-(N-sulfonylimino) and α-(N-sulfonylamino) aryl ketones to 4-hydroxy-benzo-δ- and 3-(α-hydroxy-arylmethyl)-benzo-γ-sultams is presented. By employing enantiopure ansa-Ru[PipSO2DPEN(CH2)4Ph] cat. II with S/C = 10 000 in a HCO2H/Et3N binary mix, up to >99.9% ee and dr >99:1 are obtained with 100% conversion under mild conditions. Application to access the stereopure "structurally simplified TsDPEN" N,N-ligand syn-3-(α-aminobenzyl)-benzo-γ-sultam ("syn-ULTAM") and its structural isomer trans-4-amino-3-phenyl-benzo-δ-sultam (trans-4) is demonstrated.

Synthesis and α-glucosidase inhibition activity of 2-[3-(Benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2h-benzo[e][1,2]thiazin-2-yl]-n-arylacetamides: An in silico and biochemical approach

Diabetes mellitus (DM) is a chronic disorder and has affected a large number of people worldwide. Insufficient insulin production causes an increase in blood glucose level that results in DM. To lower the blood glucose level, various drugs are employed th

Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2

Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) continues to spread worldwide, with 25 million confirmed cases and 800 thousand deaths. Effective treatments to target SARS-CoV-2 are urgently needed. In the present study, we have identified a

Synthesis and biological evaluation as well as in silico studies of arylpiperazine-1,2-benzothiazine derivatives as novel anti-inflammatory agents

Novel arylpiperazine-1,2-benzothiazine derivatives have been designed and synthesized as potential anti-inflammatory agents. Their structure and properties have been studied using spectroscopic techniques (1H NMR, 13C NMR, FT-IR), MS

Synthesis of new tricyclic 1,2-thiazine derivatives with anti-inflammatory activity

New, tricyclic compounds containing a sulfonyl moiety in their structure, as potential safer COX inhibitors, were designed and synthesized. New derivatives have three conjugated rings and a sulfonyl group. A third ring, i.e., an oxazine, oxazepine or oxaz

Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms

A large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). They were obtained by re

Discovery of (2-benzoylethen-1-ol)-containing 1,2-benzothiazine derivatives as novel 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibiting-based herbicide lead compounds

A series of (2-benzoylethen-1-ol)-containing benzothiazine derivatives was synthesized, and their herbicidal activities were first evaluated. The bioassay results indicated that some of 3-benzoyl-4-hydroxy-2-methyl-2H-1,2-benzothiazine-1,1-dioxide derivatives displayed good herbicidal activity in greenhouse testing, especially, compound 4w had good pre-emergent herbicidal activities against Brassica campestris, Amaranthus retroflexus and Echinochloa crusgalli even at a dosage of 187.5 g ha-1. More importantly, compound 4w displayed significant inhibitory activity against Arabidopsis thaliana HPPD and was identified as the most potent candidate with IC50 value of 0.48 μM, which is better than the commercial herbicide sulctrione (IC50 = 0.53 μM) and comparable with the commercial herbicide mesotrione (IC50 = 0.25 μM). The structure-activity relationships was studied and provided some useful information for improving herbicidal activity. The present work indicated that (2-benzoylethen-1-ol)-containing 1,2-benzothiazine motif could be a potential lead structure for further development of novel HPPD inhibiting-based herbicides.

Saccharin-based μ-oxo imidoiodane: A readily available and highly reactive reagent for electrophilic amination

Three new saccharin-based hypervalent iodine compounds were prepared by the reaction of saccharine with (diacetoxyiodo)arenes or acetoxybenziodoxole. Structures of these new imidoiodanes were established by X-ray crystallography. The saccharin-based μ-oxo-bridged imidoiodane readily reacts with silyl enol ethers under mild conditions to give the corresponding α-aminated carbonyl compounds in moderate yields. Sweet saccharin: Three new saccharin-derived hypervalent iodine compounds were prepared by the reaction of saccharine with (diacetoxyiodo)arenes or acetoxybenziodoxole. The saccharin-based μ-oxo-bridged imidoiodane readily reacts with silyl enol ethers to give the corresponding α-aminated carbonyl compounds in moderate yields.

Studies on synthesis of novel triazole tagged pyrazole fused naphthalene 5-thiazine-5,5-dioxide derivatives, their antimicrobial, and antioxidant activity

A series of novel triazole tagged pyrazole fused naphthalene-5-thiazine-5, 5-dioxide derivatives 8 and 9 were synthesized starting from sodium salt of saccharin 1. The structure of each intermediate and products was established on the basis of spectroscop