878671-96-6

基本信息
5-氨基-4-(4-環(huán)丙基-1-萘)-2
3-氨基-4-(4-環(huán)丙基萘-1-基)-4H-1,2,4-三唑-5-硫醇
5-氨基-4-(4-環(huán)丙基萘-1-基)-4H-3-巰基-[1,2,4]三唑
5-氨基-4-(4-環(huán)丙基萘-1-基)-4H-1,2,4-三氮唑-3-硫醇
5-氨基-4-(4-環(huán)丙基-1-萘)-2,4-二氫-3H-1,2,4-噻唑-3-硫酮
5-氨基-4-(4-環(huán)丙基-1-萘)-2,4-二氫-3H-1,2,4-噻唑-3-硫醇
5-氨基-4-(4-環(huán)丙基萘-1-基)-2,4-二氫-3H-1,2,4-三唑-3-硫酮
5-氨基-4-(4-環(huán)丙基-1-萘基)-2,4-二氫-3H-1,2,4-三唑-3-硫酮
5-氨基-4-(4-環(huán)丙基-1-萘)-2,4二氫-3H-1,2,4-噻唑-3-硫醇 痛風(fēng)藥LESINURAD (RDEA-594)中間體
3H-1,2,4-Triazole-3-thione, 5-amino-4-(4-cyclopropyl-1-napht...
3-Amino-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazole-5-thiol
3-Amino-4-(4-cyclopropyl-1-naphthyl)-1H-1,2,4-triazole-5(4H)-thione
3-amino-4-(4-cyclopropylnaphthalen-1-yl)-1H-1,2,4-triazole-5-thione
3-Amino-4-(4-cyclopropylnaphthalen-1-yl)-1H-1,2,4-triazole-5(4H)-thione
3-amino-4 - (4-cyclopropylnaphthalene - 1-yl) -1H-1,2, 4-triazole-5-thione
3H-1,2,4-Triazole-3-thione, 5-amino-4-(4-cyclopropyl-1-phthalenyl)-2,4-dihydro
5-amino-4-(4-cyclopropylnaphthalen-1-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione
5-amino-4-(4-cyclopropyl-1-naphthalenyl)-2,4-dihydro-3H-1,2,4-Triazole-3-thione
物理化學(xué)性質(zhì)
制備方法

878671-95-5

1937-19-5

878671-96-6
以1-環(huán)丙基-4-異硫氰酸酯基萘(13.3 mmol,3.0 g)和氨基胍鹽酸鹽(26.6 mmol,2.9 g)為原料,在50 mL N,N-二甲基甲酰胺中混合。在攪拌條件下,緩慢加入N,N-二異丙基乙胺(39.9 mmol,5.1 g)。將反應(yīng)混合物在室溫下攪拌反應(yīng)50±12小時。反應(yīng)完成后,通過旋轉(zhuǎn)蒸發(fā)儀除去溶劑至干燥。向殘留物中加入20 mL 2M氫氧化鈉溶液,繼續(xù)反應(yīng)50±12小時。反應(yīng)終止后,過濾反應(yīng)混合物,濾液用稀鹽酸調(diào)節(jié)至pH=4,此時觀察到大量白色沉淀生成。收集沉淀,用去離子水洗滌,隨后在45-50℃下真空干燥,得到中間體化合物5-氨基-4-(4-環(huán)丙基-1-萘)-2,4-二氫-3H-1,2,4-三唑-3-硫醇(VI),產(chǎn)量2.85 g,收率76%。
參考文獻:
[1] Patent: CN105566237, 2016, A. Location in patent: Paragraph 0066; 0067; 0068
[2] Patent: WO2009/70740, 2009, A2. Location in patent: Page/Page column 89-90
[3] Patent: WO2006/26356, 2006, A2. Location in patent: Page/Page column 21
[4] Patent: WO2011/85009, 2011, A2. Location in patent: Page/Page column 37