Citation: Hong-Jun Yang, Fang-Jun Xiong, Jie Li, Fen-Er Chen. A family of novel bifunctional organocatalysts：Highly enantioselective alcoholysis of meso cyclic anhydrides and its application for synthesis of the key intermediate of P2X₇ receptor antagonists[J]. Chinese Chemical Letters, ;2013, 24(07): 553-558. shu

A family of novel bifunctional organocatalysts：Highly enantioselective alcoholysis of meso cyclic anhydrides and its application for synthesis of the key intermediate of P2X₇ receptor antagonists

1.
a Department of Chemistry, Fudan University, Shanghai 200433, China;
2.
b Institute of Biomedical Science, Fudan University, Shanghai 200433, China

Corresponding author: Fen-Er Chen,
Received Date: 21 February 2013
Available Online: 2 April 2013

A family of novel squaramides/sulfamides based on 1,2-alkamine was developed as chiral bifunctional catalysts to promote the asymmetric alcoholysis of meso cyclic anhydrides. The hemiesters were obtained in high yield with up to 93% ee. The usefulness of this methodology was demonstrated in the asymmetric synthesis of the key intermediate of P2X₇ receptor antagonists.
- Asymmetric alcoholysis,
- Bifunctional organocatalyst,
- Cyclic anhydrides,
- P2X₇ receptor antagonists,
- Sulfamides
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通讯作者: 陈斌, bchen63@163.com

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沈阳化工大学材料科学与工程学院沈阳 110142

A family of novel bifunctional organocatalysts：Highly enantioselective alcoholysis of meso cyclic anhydrides and its application for synthesis of the key intermediate of P2X7 receptor antagonists

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通讯作者: 陈斌, bchen63@163.com

A family of novel bifunctional organocatalysts：Highly enantioselective alcoholysis of meso cyclic anhydrides and its application for synthesis of the key intermediate of P2X₇ receptor antagonists