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. 2005 Apr 15;15(8):1979-82.
doi: 10.1016/j.bmcl.2005.02.071.

Synthesis of the optical isomers of a new anticholinergic drug, penehyclidine hydrochloride (8018)

Xiang-Yu Han  1 , He Liu, Chun-He Liu, Bo Wu, Lan-Fu Chen, Bo-Hua Zhong, Ke-Liang Liu
Affiliations

Synthesis of the optical isomers of a new anticholinergic drug, penehyclidine hydrochloride (8018)

Xiang-Yu Han et al. Bioorg Med Chem Lett. .

Abstract

A practical diastereoselective synthetic method for 8018 enantiopure isomers is described. The intramolecular asymmetric epoxidation of mono-sulfonate 4 was applied for the execution of the synthesis of the key chiral building block for the first time. The isomers were obtained with 70-76% yields in 99-100% ee.

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