Asymmetric total synthesis of (S)-dapoxetine

作者：Kim Sun Joo; Jeon Tae Hong; Min Im Sook; Kim In Su^*; Jung Young Hoon

来源：Tetrahedron Letters, 2012, 53(28): 3680-3682.

DOI：10.1016/j.tetlet.2012.05.037

• Dapoxetine
• Chlorosulfonyl isocyanate
• Amination
• Asymmetric

A concise asymmetric total synthesis of (S)-dapoxetine from commercially available 3-chloropropiophenone is described. The key step includes a highly stereoselective amination of chiral benzylic ether, with the retention of stereochemistry, using chlorosulfonyl isocyanate.

• 出版日期2012-7-11