Patent · US Active

Synthesis of cyclic amidines

US8598346B2 · kind B2 · utility

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1References

15Claims

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Assignee

BITOP AG · DE

Inventors

Georg Lentzen · Geleen, NL
Thorsten Neuhaus · Biberach an der Riß, DE

Key dates

Filing date	Jul 16, 2009
Grant date	Dec 3, 2013
Priority date	—
Expiry date	Dec 11, 2029

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07D243/04
WIPO fieldOrganic fine chemistry
WIPO sectorChemistry

Abstract

The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a β-, γ- or δ-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.