1788-08-5

基本信息
對(duì)乙炔基苯磺酰胺
4-乙炔基苯磺酰胺
4-ethynylbenzenesulfonamide
BenzenesulfonaMide, 4-ethynyl-
4-ethynylbenzene-1-sulfonaMide
4-Ethynylbenzenesulfonamide >
Benzenesulfonamide, 4-ethynyl- (9CI)
物理化學(xué)性質(zhì)
制備方法

775331-26-5

1788-08-5
在氮?dú)獗Wo(hù)下,將步驟1中制得的4-((三甲基甲硅烷基)乙炔基)苯磺酰胺(1.69 g,3.13 mmol)溶于無(wú)水四氫呋喃中,加入四丁基氟化銨(TBAF,10 mL,1.0 M的四氫呋喃溶液,10 mmol)。將反應(yīng)混合物于室溫下攪拌。通過(guò)硅膠薄層色譜(TLC,展開劑比例為1:1的己烷:乙酸乙酯)監(jiān)測(cè)反應(yīng)進(jìn)程。反應(yīng)完成后,加入10%鹽酸和乙酸乙酯。分離有機(jī)層,依次用水和氯化銨水溶液洗滌兩次,無(wú)水硫酸鈉干燥,減壓濃縮,得到目標(biāo)產(chǎn)物4-炔基苯磺酰胺0.748 g,產(chǎn)率62%。高分辨電噴霧質(zhì)譜(ESHRMS)測(cè)得m/z為199.0506([M+NH4]+,C8H7NO2SNH4的計(jì)算值為199.0541)。
參考文獻(xiàn):
[1] MedChemComm, 2018, vol. 9, # 3, p. 534 - 544
[2] Patent: WO2004/87686, 2004, A2. Location in patent: Page 229
[3] Patent: WO2004/87687, 2004, A1. Location in patent: Page 229
[4] Organic and biomolecular chemistry, 2003, vol. 1, # 3, p. 498 - 506
[5] Bioorganic and Medicinal Chemistry, 2008, vol. 16, # 4, p. 1948 - 1956