767340-03-4
767340-03-4 結(jié)構(gòu)式
基本信息
(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氫-[1,2,4]三唑并[4,3-A]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)-2-丁烯胺
(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氫-[1,2,4]三唑并[4,3-A]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)丁-2-烯-2-胺
(2Z)-3-Amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-α]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-2-buten-1-one
(2Z)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-α]pyrazin -7(8H)-yl]-1-(2,4,5-trifluorophenyl)but-2-en-2-amine
(2Z)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]
(2Z)-3-Amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-2-buten-1-one
(2Z)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)but-2-en-2-amine
(2Z)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine-7(8H)-yl]-1-(2,4,5-trifluorophenyl)but-2-en-2-amine
物理化學(xué)性質(zhì)
制備方法
![(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氫-[1,2,4]三唑并[4,3-a]吡嗪-7-(8H)-基]-1-(2,4,5-三氟苯基)丁-2-酮](/CAS/GIF/764667-65-4.gif)
764667-65-4
767340-03-4
實(shí)施例1：制備(Z)-3-氨基-1-(3-(三氟甲基)-5,6-二氫-[1,2,4]三唑并[4,3-a]吡嗪-7(8H)-基)-4-(2,4,5-三氟苯基)丁-2-烯-1-酮。將4-氧代-4-[3-(三氟甲基)-5,6-二氫-[1,2,4]三唑并[4,3-a]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)丁-2-酮（427.0g，根據(jù)US 7,326,708 B2或J. Am. Chem. Soc. 2009制備）與甲醇（1000ml）混合，在25-30℃下通入干燥氨氣（53.6g）。隨后將反應(yīng)混合物加熱至回流（60-65℃），并在此溫度下維持反應(yīng)3.0-4.0小時。反應(yīng)完成后，將混合物冷卻至0-5℃，過濾收集沉淀的固體，并用冷甲醇洗滌。濕濾餅在60-65℃下干燥，得到340.0g目標(biāo)產(chǎn)物(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氫-[1,2,4]三唑并[4,3-a]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)丁-2-烯-2-胺，摩爾產(chǎn)率為79.8%，HPLC純度為98.99%。
參考文獻(xiàn)：
[1] Journal of the American Chemical Society, 2009, vol. 131, # 25, p. 8798 - 8804
[2] Patent: WO2016/110750, 2016, A1. Location in patent: Page/Page column 15; 16
[3] Patent: WO2004/85378, 2004, A1. Location in patent: Page 16
[4] Patent: WO2005/97733, 2005, A1. Location in patent: Page/Page column 23-24
[5] Patent: WO2006/81151, 2006, A1. Location in patent: Page/Page column 14; 15