Short Protecting Group-free Syntheses of CDE Synthon of Racemic Camptothecin

Author:

Shao Pingxuan1,Lu Wei1,Wang Lei1

Affiliation:

1. Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China

Abstract

A practical and concise total synthesis of tricyclic ketone 7 (CDE ring), a valuable intermediate for the synthesis of racemic camptothecin and analogs, was described (8 chemical steps and 29% overall yield). The synthesis starts with two inexpensive, readily available materials and is operationally simple to perform. It is worth mentioning that the reported protecting group-free synthesis, with advantages of a short route, would be helpful for the future development of industry-scale syntheses of camptothecin-family alkaloids.

Funder

China Postdoctoral Science Foundation

Publisher

Bentham Science Publishers Ltd.

Subject

Organic Chemistry,Biochemistry

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