Abstract

Asymmetric synthesis of N-(2-chloro-5-methylthiophenyl)- N′-(3-methylsulfinylphenyl)- N′-methylguanidine (CNS 5788) was achieved in high enantiomeric excess through condensation of the cyanamide derivative, 6 and the sulfinylaniline hydrochloride, 5. The key step involved the asymmetric oxidation of N-methyl-3-methylthioaniline using a Davis reagent.

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