944804-88-0

基本信息
4-溴噻唑-2-甲胺叔丁酯
2-叔丁氧羰基胺基-4-溴噻唑
2-N-BOC-氨基-4-溴噻唑
2-(BOC-氨基)-4-溴噻唑
(4-溴噻唑-2-基)氨基甲酸叔丁酯
2-(Boc-amino)-4-bromothiazole
tert-Butyl 4-bromothiazol-2-ylcarbamate
tert-Butyl N-(4-bromothiazol-2-yl)carbamate
Tert-butyl N-(4-broMo-1,3-thiazol-2-yl)carbaMate
(4-Bromo-thiazol-2-yl)-carbamic acid tert-butyl ester
Carbamic acid, N-(4-bromo-2-thiazolyl)-, 1,1-dimethylethyl ester
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表

405939-39-1

944804-88-0
以N-BOC-2-氨基-5-溴噻唑?yàn)樵虾铣?-溴噻唑-2-甲胺叔丁酯的一般步驟:在0℃下,將二異丙胺(2.3 mL,16 mmol)溶于30 mL THF中。向此溶液中緩慢加入2.5 M丁基鋰的己烷溶液(6.4 mL,16 mmol),并在相同溫度下攪拌反應(yīng)混合物20分鐘。隨后,將5-溴噻唑-2-基氨基甲酸叔丁酯(1.5 g,5.4 mmol)溶于8 mL THF中,緩慢滴加到反應(yīng)體系中。反應(yīng)15分鐘后,加入約2 mL水淬滅反應(yīng),并將混合物逐漸升溫至室溫,繼續(xù)攪拌12小時(shí)。反應(yīng)完成后,用30 mL 1/2飽和NH4Cl水溶液稀釋反應(yīng)混合物,轉(zhuǎn)移至分液漏斗中。用5 mL EtOAc萃取兩次,合并有機(jī)相,用鹽水洗滌,經(jīng)MgSO4干燥。過(guò)濾后,減壓濃縮有機(jī)相,得到4-溴噻唑-2-基氨基甲酸叔丁酯(1.5 g,收率100%),為棕色固體。
參考文獻(xiàn):
[1] Patent: US2007/173506, 2007, A1. Location in patent: Page/Page column 61; 62
[2] Patent: WO2010/83246, 2010, A1. Location in patent: Page/Page column 123
[3] Patent: US2009/36467, 2009, A1. Location in patent: Page/Page column 64; 72; 73
[4] Patent: US2012/108591, 2012, A1. Location in patent: Page/Page column 29
[5] European Journal of Medicinal Chemistry, 2018, vol. 158, p. 896 - 916