6223-35-4

基本信息
呱侖酸鈉
奧磺酸鈉
薁磺酸鈉
瓜拉酸鈉
愈創(chuàng)木磺酸鈉
愈創(chuàng)木薁磺酸鈉
7-異丙基-1
愈創(chuàng)木奧磺酸鈉
薁磺酸鈉,愈創(chuàng)木薁磺酸鈉
SODIUM GUAIAZULENE SULFONATE
sodium gualenate
3-Sulfonate sodium salt
Azulene sulfonate sodium
Sodium guazulene sulfonate
Guaiazulenesulfonate sodium
guaiazulene / azulene powder
Sodium azulene sulphonate, 98%
Sodium 1,4-dimethyl-7-isopropylazulene-3-sulfonate
物理化學(xué)性質(zhì)
制備方法

489-84-9

6223-35-4
(1) 制備3,8-二甲基-5-異丙基甘菊-1-磺酸鈉 在冰浴條件下,向25 mL梨形燒瓶中加入4 mmol愈創(chuàng)木酚和2 mL乙酸酐(Ac2O)。隨后,通過恒壓滴液漏斗(頂部裝有干燥管)緩慢滴加1 mL濃硫酸(H2SO4)和2 mL乙酸酐(Ac2O)的混合物。滴加完畢后,將反應(yīng)混合物在室溫下攪拌約2小時,期間通過薄層色譜(TLC)監(jiān)測反應(yīng)進(jìn)度,直至原料完全消失。反應(yīng)完成后,將混合物溶液倒入4 mL水中,并滴加氫氧化鈉(NaOH)溶液調(diào)節(jié)pH至8-9。隨后,將混合物溶液冷卻以促進(jìn)沉淀形成,進(jìn)行抽濾,依次用冷水和石油醚洗滌沉淀,干燥后得到1.05 g藍(lán)色固體產(chǎn)物。產(chǎn)率為87.5%,熔點為106-107℃。
參考文獻(xiàn):
[1] Patent: US2014/206741, 2014, A1. Location in patent: Paragraph 0108-0110
[2] Bioorganic and Medicinal Chemistry, 2016, vol. 24, # 8, p. 1653 - 1657
[3] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 19, p. 5722 - 5725
[4] Chemical Biology and Drug Design, 2016, p. 264 - 271
常見問題列表
薁磺酸鈉不穩(wěn)定,受光照,空氣氧化和高溫環(huán)境下會分解,易脫去磺酸基。根據(jù)現(xiàn)有報道,薁磺酸鈉含有半個或一個結(jié)晶水均是常見情況。
薁磺酸鈉是洋甘菊花的有效成分,具有很強(qiáng)的抗胃蛋白酶、消炎、抗菌、抗過敏、促進(jìn)粘膜新城代謝的作用,主要用于研究十二指腸潰瘍,胃潰瘍和胃炎。
Sodium gualenate is an unstable compound, which is gradually decomposed in the solid state at room temperature. When heated, Sodium gualenate decomposes almost completely within 1 week. It was found that a kneaded mixture of Sodium gualenate and cornstarch (weight ratio; 1:250) for tableting with water is stable. So, during production, Sodium gualenate could be stabilized using water. Sodium gualenate slightly inhibits the histamine release from rat peritoneal mast cells and strongly inhibits the leukocyte emigration induced by fMLP.
Sodium gualenate has been frequently used for the treatment of human gastritis. Cytoprotection is defined as the main mechanism of Sodium gualenate to protect the mucosa of the stomach and the antipeptic actions in vivo have also been shown.