An efficient asymmetric synthesis of the potent beta-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity

作者：Baker James R^*; Hothersall J Daniel; Fitzmaurice Richard J; Tucknott Matthew; Vinter Andy; Tinker Andrew; Caddick Stephen

来源：Chemical communications, 2010, 46(22): 3953-3954.

DOI：10.1039/c0cc00142b

A highly efficient, practical and. flexible two-step asymmetric synthesis of the beta(2)-selective beta-blocker ICI 118,551 is reported, allowing an unambiguous determination of the dependency of biological activity with optical activity, revealing the S,S-enantiomer to be the most potent.

• 出版日期2010