110256-15-0

基本信息
5-環(huán)丙基異F唑-3-羧酸
5-環(huán)丙基異噻唑-3-羧酸
5-環(huán)丙基異噁唑-3-甲酸
5-環(huán)丙基異噁唑-3-羧酸
5-環(huán)丙基異惡唑-3-羧酸
5-環(huán)丙基-3-異惡唑甲酸
5-環(huán)丙基-1,2-惡唑-3-羧酸
5-cyclopropyl-3-isoxazolecarboxylic acid
3-Isoxazolecarboxylicacid, 5-cyclopropyl-
3-Isoxazolecarboxylicacid,5-cyclopropyl-(9CI)
5-cyclopropylisoxazole-3-carboxylic acid(SALTDATA: FREE)
物理化學(xué)性質(zhì)
制備方法

21080-81-9

110256-15-0
以5-環(huán)丙基異噁唑-3-甲酸乙酯為原料合成5-環(huán)丙基異惡唑-3-羧酸的一般步驟如下:中間體16-制備5-環(huán)丙基異惡唑-3-羧酸。將5-環(huán)丙基異惡唑-3-羧酸乙酯(0.550 g, 3.04 mmol)與1M氫氧化鈉水溶液(9.11 mL, 9.11 mmol)的混合物在室溫下攪拌72小時(shí)。反應(yīng)完成后,用6N鹽酸將反應(yīng)液的pH調(diào)節(jié)至1,隨后用乙酸乙酯進(jìn)行萃取。分離有機(jī)層,用無水硫酸鎂干燥,減壓濃縮,得到5-環(huán)丙基異惡唑-3-羧酸固體0.446 g,收率96%。產(chǎn)物經(jīng)質(zhì)譜分析確認(rèn):ESI/APCI(+) m/z: 154 (M+H), 176 (M+Na); ESI/APCI(-) m/z: 152 (M-H)。
參考文獻(xiàn):
[1] Journal of Medicinal Chemistry, 2016, vol. 59, # 1, p. 358 - 373
[2] Patent: WO2010/142801, 2010, A1. Location in patent: Page/Page column 151
[3] Patent: US2003/236287, 2003, A1. Location in patent: Page 46, 47
[4] Patent: WO2016/40502, 2016, A1. Location in patent: Page/Page column 65
[5] Patent: WO2016/40504, 2016, A1. Location in patent: Paragraph 0194