110380-99-9

Upstream product

• 110417-59-9 N-<(1-bromo-2-phenylethenyl)sulfonyl>morpholine 
• 1697-34-3 4-methanesulfonylmorpholine 
• 55129-82-3 1-bromo-2-phenylethenesulfonyl chloride 
• 52147-97-4 trans 2-phenylethenesulfonyl chloride 
• 17299-32-0 (E)-4-<(2-phenylethynyl)sulfonyl>morpholine 
• 22457-12-1 4-((bromomethyl)sulfonyl)morpholine 
• 146301-47-5 4-<(phenylethynyl)sulfinyl>morpholine 
• 110417-55-5 N-[(2-Phenyloxo-2-ethane)sulphonyl]morpholine 

Downstream Products

• 1041424-65-0 C₃₇H₄₉FN₂O₇S 
• 845281-70-1 C₃₇H₄₉FN₂O₇S 
• 110381-01-6 4-((2S,3R)-3-Phenyl-oxiranesulfonyl)-morpholine 
• 110417-55-5 N-[(2-Phenyloxo-2-ethane)sulphonyl]morpholine 
• 110381-12-9 4-((Z)-2-Phenyl-ethenesulfonyl)-morpholine 

Relevant academic research and scientific papers

Hepatoselectivity of statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors

4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3 + 2] cycloaddition of a Muenchnone with a sulfonamide-substituted alkyne. We identified compounds with greater selectivity for hepatocytes compared to L6-myocytes than rosuvastatin and atorvastatin. There was an inverse correlation of myocyte potencies and C log P values. A number of analogs were effective at reducing cholesterol in acute and chronic in vivo models but they lacked sufficient chronic in vivo activity to warrant further development.

Preparation of N,N-disubstituted (1-alkyne)- and (E)-(1-alkene)-sulfinamides and their conversion into the corresponding sulfinates or sulfonamides

Treatment of (1-piperidine)- or (4-morpholine)-sulfinyl chloride with unsaturated lithio, bromomagnesio or diisobutylalumino derivatives afforded the title sulfinamides 3 and 5.The 1-alkynesulfinamides 3 were smoothly reduced with lithium aluminium hydrid

A simple and versatile synthesis of substituted ethynesulfonamides

A variety of substituted 2-arylethynesulfonamides were prepared by a two-step sequence: 1. preparation of 2-oxo-2-arylethanesulfonamides by reaction of the appropriate methanesulfonamide carbanion with a substituted benzoic ester, 2. dehydration of the re

New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides

Two series of 2-substituted 1,2-epoxyethanesulfonamides 2 and ethynesulfonamides 5 were synthesized and evaluated for their antifilarial activity. The trans epoxides 2T were stereospecifically prepared by a Darzens reaction between aldehydes and halomethanesulfonamides. The cis isomers 2c were obtained from ethynesulfonamides 5 by semihydrogenation followed by KOCl epoxidation. 2-Substituted ethynesulfonamides 5 were synthesized from appropriate trans-ethenesulfonamides by a bromination/dehydrobromination sequence. These products, as well as several synthetic intermediates, were evaluated for antifilarial activity against Molinemia dessetae either in vivo in its natural host, the rodent Proechimys oris, or in vitro by a new test using cultures of the infective larvae. Most of the epoxides 2T and acetylenic derivatives 5 bearing a 2-aryl substituent were active in vitro. Among these compounds, four epoxides 2T and one acetylenic derivative 5 showed marked macrofilaricidal activity in vivo without any microfilaricidal activity. The differences between the in vivo and in vitro results may be due, in part, to the low chemical stability of the epoxy sulfonamides 2T. Despite this limitation, the activities observed in this reliable animal model suggest further development and testing of both series 2T and 5 as macrofilaricides.