化学合成。
化学合成
合成路线 1(1. 合成:4441-30-9)
产率:96%
合成条件:With potassium carbonate In toluene at 75 - 80℃; for 8 h;
实验步骤:向反应瓶中加入913.5g甲苯,174g吗啉和556g 3-溴丙醇,并在搅拌下加入331.2g碳酸钾。将反应在75-80℃下加热8小时。 反应完成后,加压过滤并浓缩滤液,除去甲苯和未反应的原料,得到淡黄色278.4克N - (3-羟丙基)吗啡,摩尔产率96%,纯度为98.5%。
参考文献:
- [1] Patent: CN106045942, 2016, A. Location in patent: Paragraph 0023; 0020 [2] Patent: CN103382206, 2016, B. Location in patent: Paragraph 0235-0238 [3] Journal of Medicinal Chemistry, 2004, vol. 47, # 4, p. 871 - 887 [4] Patent: WO2004/108677, 2004, A1. Location in patent: Page 141 [5] Patent: US6265411, 2001, B1 [6] Patent: US6291455, 2001, B1 [7] Patent: US6294532, 2001, B1 [8] Patent: EP1171440, 2004, B1. Location in patent: Page 50