| A facile enantioselective synthesis of (+)-rolipram via C-H insertion process |
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| 基金项目： | Supported by the National Science Foundation of China (Grant No. 20202011) and the Chinese
Academy of Sciences |
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| 摘 要： | Rolipram, (±)-4-(3-cyclopentyloxyl-4-methoxylphenyl)-2-pyrrolidinone,is known as a potent and selective inhibitor of phosphodiesterase type IV(PDE IV)1.In fact, although both enantiomers are active, the levorotatory isomer, for which several synthesis has been recently reported2, has proved to be the most active one. Hashimoto and Jung have repored rolipram,s synthesis via intramolecular C-H insertion reaction of α-methoxylcarbonyl-α-diazoacetamide and α-phenylsulfonyl-α-diazoacetamid…
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A facile enantioselective synthesis of (+)-rolipram via C-H insertion process |
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| Authors: | LIU Wei-jun CHEN Zhen-liang WANG Yuan-hua HU Qing-quan HUANG Hao-Xi CHEN Zhi-yong HU Wen-Hao |
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| Abstract: | Rolipram, (±)-4-(3-cyclopentyloxyl-4-methoxylphenyl)-2-pyrrolidinone,is known as a potent and selective inhibitor of phosphodiesterase type Ⅳ(PDE Ⅳ)1.In fact, although both enantiomers are active, the levorotatory isomer, for which several synthesis has been recently reported2, has proved to be the most active one. Hashimoto and Jung have repored rolipram's synthesis via intramolecular C-H insertion reaction of α -methoxylcarbonyl- α -diazoacetamide and α-phenylsulfonyl-α-diazoacetamide3,4. Based on the discovery of the excellent N-protecting group:cumyl, we have now explored a new and facile route to 1 |
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| Keywords: | Rolipram enantioselective synthesis C-H insertion N-cumyl chiral dirhodium(Ⅱ)carboxamide |
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