1533519-85-5

基本信息
雷西那德雜質(zhì)11
雷西納德中間體1
蕾西納德原料及其中間體
LESINURAD雜質(zhì)9
LESINURAD中間體4
LESINURAD中間體1
4-三唑-3-基]硫基]乙酸甲酯
2-[[4-(4-環(huán)丙基萘-1-基)-4H-1
2-(4-(4-環(huán)丙基萘-1-基)-4H-1,2,4-噻唑-3-硫基)乙酸甲酯
LSEINURAD INT
Lesinurad INT4
Lesinurad internate 4
Intermediate of lesinurad
4-triazol-3-yl]thio]acetate
Pentanedioicacid,5-oxo-,dimethylester
Methyl 2-[[4-(4-cyclopropylnaphthalen-1-yl)-4H-1
Acetic acid, 2-((4-(4-cyclopropyl-1-naphthalenyl)-4H-1,2,4-t...
Methyl 2-[[4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl]thio]acetate
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表

1533519-84-4

96-32-2
![2-[[4-(4-環(huán)丙基萘-1-基)-4H-1,2,4-三唑-3-基]硫基]乙酸甲酯](/CAS/20150408/GIF/1533519-85-5.gif)
1533519-85-5
在裝有磁力攪拌器和溫度計(jì)的100 mL三頸圓底燒瓶中,加入25 mL N,N-二甲基甲酰胺(DMF)和中間體(III)(2.67 g,1-環(huán)丙基-4-異硫代氰?;粒?。在室溫下攪拌至完全溶解后,依次加入碳酸鉀(1.45 g)和溴乙酸甲酯(1.61 g)。控制反應(yīng)溫度在25℃,緩慢滴加完畢后,繼續(xù)攪拌反應(yīng)3小時(shí)。反應(yīng)完成后,向反應(yīng)混合物中加入50 mL水稀釋?zhuān)S后用乙酸乙酯(50 mL × 3)進(jìn)行萃取。合并有機(jī)相,用旋轉(zhuǎn)蒸發(fā)儀濃縮除去乙酸乙酯。向濃縮后的殘余物中加入50 mL甲醇,加熱至回流使晶體溶解,隨后緩慢冷卻至室溫進(jìn)行重結(jié)晶。通過(guò)抽濾收集晶體,并用少量冷甲醇洗滌,真空干燥后得到中間體(IV)(2-((4-(4-環(huán)丙基萘-1-基)-4H-1,2,4-三唑-3-基)硫代)乙酸甲酯)3.22 g,產(chǎn)率99.5%。
參考文獻(xiàn):
[1] Patent: CN105906576, 2016, A. Location in patent: Paragraph 0070; 0071; 0083; 0084
[2] Patent: WO2014/8295, 2014, A1. Location in patent: Paragraph 0254-0262
[3] Patent: CN105399694, 2016, A. Location in patent: Paragraph 0085; 0086; 0087; 0088
[4] Patent: CN107098866, 2017, A. Location in patent: Paragraph 0079; 0080; 0081; 0082; 0083