5-FLUOROBENZO-[2,1,3]-THIADIAZOLE synthesis
- Product Name:5-FLUOROBENZO-[2,1,3]-THIADIAZOLE
- CAS Number:17821-75-9
- Molecular formula:C6H3FN2S
- Molecular Weight:154.16
Yield: 74%
Reaction Conditions:
in toluene for 16 h;Reflux;
Steps:
A.3.1 Step-1: Synthesis of 5-fluorobenzo[c][1 ,2,5]thiadiazole X-3a:Step-1: Synthesis of 5-fluorobenzo[c][1 ,2,5]thiadiazole X-3a:
To a solution of 4-fluorobenzene-1 ,2-diamine (1.50 g, 11.9 mmol) in toluene (20 ml) wasadded (sulfinylamino)benzene (0.40 ml, 35.7 mmol) and the reaction mixture was heated5 to reflux for 16h. Progress of the reaction was monitored by TLC and LCMS. Aftercompletion, the reaction mixture was concentrated under vacuum. The residue wasdiluted with H20 (150 ml) and extracted with EtOAc (3 x 150 ml). The organic layer wasseparated, dried over anhydrous Na2S04 and concentrated under vacuum. The crudeobtained was purified by flash column chromatography (0 to 3% EtOAc in hexanes) to10 afford 1.36g of 5-fluoro-2, 1 ,3-benzothiadiazole X-3a as a light yellow liquid.Yield: 74%.1H NMR (400 MHz, DMSO-d6) o 7.67-7.73 (m, 1H) 7.92-7.95 (m, 1H) 8.15-8.19 (m, 1H
References:
UCB PHARMA GMBH;MUELLER, Christa E.;PEGURIER, Cécile;DELIGNY, Michael Louis Robert;EL-TAYEB, Ali;HOCKEMEYER, Joerg;LEDECQ, Marie;MERCIER, Jo?l;PROVINS, Laurent;BOSHTA, Nader M.;BHATTARAI, Sanjay;NAMASIVAYAM, Vigneshwaran;FUNKE, Mario;SCHWACH, Lukas;GOLLOS, Sabrina;VON LAUFENBERG, Daniel;BARRé, Ana?s WO2018/122232, 2018, A1 Location in patent:Page/Page column 202; 203
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