A straightforward and efficient synthesis of praziquantel enantiomers and their 4鈥?hydroxy derivatives

详细信息    查看全文

• 作者：Alberto Cedillo-Cruz ; Mar铆a Isabel Aguilar ; Marcos Flores-Alamo ; Francisca Palomares-Alonso ; Helgi Jung-Cook
• 刊名：Tetrahedron: Asymmetry
• 出版年：31 January, 2014
• 年：2014
• 卷：25
• 期：2
• 页码：133-140
• 全文大小：1000 K

文摘

A new method for the synthesis of praziquantel enantiomers via resolution of praziquanamine with (S)-(+)-naproxen was developed. The four 4鈥?hydroxy derivatives were obtained through each single praziquanamine enantiomer, coupling with cis- and trans-4-(benzyloxy)cyclohexanecarboxylic acids and subsequent hydrogenolysis for the deprotection of the 4鈥?OH cyclohexane residue. Additionally, the in vitro cysticidal activity of the compounds was tested, finding that (R)-(鈭?-praziquantel is the eutomer.