期刊文献+

Synthesis of(S) and(R)-tilisolol hydrochloride

Synthesis of(S) and(R)-tilisolol hydrochloride
下载PDF
导出
摘要 Tilisolol hydrochloride 1, a non-selective β-adrenoceptor blocker, was developed as a drug for the treatment of hypertension and angina pectoris. The optical active forms of 1, la and lb were synthesized from inexpensive phthalic anhydride 2 in eight steps with 13% (S) and 15% (R) overall yield. Tilisolol hydrochloride 1, a non-selective β-adrenoceptor blocker, was developed as a drug for the treatment of hypertension and angina pectoris. The optical active forms of 1, la and lb were synthesized from inexpensive phthalic anhydride 2 in eight steps with 13% (S) and 15% (R) overall yield.
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2009年第6期648-650,共3页 中国化学快报(英文版)
基金 supported by the National Natural Science Foundation of China(No.30672537)
关键词 Tilisolol hydrochloride OPTICAL SYNTHESIS Tilisolol hydrochloride Optical Synthesis
  • 相关文献

参考文献8

  • 1M. Fosset, J.R. Dewille, R.D. Green, et al. J. Biol. Chem. 263 (1988) 7933.
  • 2S. Takagif Y. Kihara, T. Mitsuiye, et al. Cardiovas. Drug Rev. 1"6 (1998) 105.
  • 3T. Imaizumi, A. Takeshita, N. Nakamura, et al. Arzneimittelforschung 38 (1988) 1342.
  • 4E.L. Eliel, A.W. Burgstahler, J. Amer. Chem. Soc. 71 (1943) 2251.
  • 5J.G. Lombardino, J. Heterocycl. Chem. 10 (1970) 1057.
  • 6J.E O'Connell, J. Parquette, W.E. Yelle, et al. Synthesis 10 (1988) 767.
  • 7Y.G. Yao, CN 101255135A.
  • 8This approach was not economical because of multiple column chromatography and low overall yield (23-30% from isoquinolin derivate 6). Moreover, this literature had not reported optical analytic data of the oxirane intermediates 7a and 7b and two optical isomers la and lb, such as optical rotation and value of ee%.

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部