287193-01-5

基本信息
3-乙炔氮雜丁烷-1-羧酸叔丁酯
3-炔基-1-氮雜環(huán)丁烷甲酸叔丁酯
3-乙炔基-1-氮雜環(huán)丁烷甲酸叔丁酯
1-BOC-3-甲基氮雜環(huán)丁烷,95%
1-Boc-3-methylazetidine,95%
tert-butyl 3-ethynylazetidine-1-carboxylate
3-Ethynyl-1-azetidinecarboxylic acid tert-butyl ester
1-Azetidinecarboxylic acid, 3-ethynyl-, 1,1-dimethylethyl ester
物理化學(xué)性質(zhì)
制備方法

177947-96-5

90965-06-3

287193-01-5
在0℃下,向3-甲?;s環(huán)丁烷-1-羧酸叔丁酯(1.3g,27mmol)在甲醇(70ml)中的攪拌溶液中加入(1-重氮基-2-氧代丙基)膦酸二甲酯(6g,31.2mmol),隨后加入碳酸鉀(14.92g,108mmol)。將反應(yīng)混合物在0℃下攪拌3小時。反應(yīng)完成后,用乙酸乙酯(150ml)稀釋反應(yīng)混合物,過濾并減壓濃縮,得到粗產(chǎn)物。粗產(chǎn)物通過快速色譜法(硅膠,洗脫劑:0-100%乙酸乙酯的己烷溶液)純化,得到3-炔基-1-氮雜環(huán)丁烷甲酸叔丁酯(4.6g,94%)。1H NMR (400MHz, DMSO-d6) δ 1.34 (s, 9H), 3.22-3.23 (m, 1H), 3.34-3.39 (m, 1H), 3.68 (t, J = 6.8Hz, 2H), 4.04 (t, J = 8.4Hz, 2H)。
參考文獻(xiàn):
[1] Patent: WO2014/165075, 2014, A1. Location in patent: Page/Page column 46; 47
[2] Patent: WO2016/4413, 2016, A2. Location in patent: Paragraph 0279
[3] Patent: US2018/86709, 2018, A1. Location in patent: Paragraph 0358-0359
[4] Patent: WO2015/51244, 2015, A1. Location in patent: Paragraph 00655; 00709
[5] Patent: WO2016/105485, 2016, A2. Location in patent: Paragraph 0219