The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 03, 2013

Filed:

Jul. 16, 2009
Applicants:

Georg Lentzen, Wesel, DE;

Thorsten Neuhaus, Bochum, DE;

Inventors:

Georg Lentzen, Wesel, DE;

Thorsten Neuhaus, Bochum, DE;

Assignee:

Bitop AG, , DE;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61P 17/00 (2006.01); A61K 31/505 (2006.01); C07D 233/18 (2006.01); C07D 239/06 (2006.01); C07D 243/04 (2006.01);
U.S. Cl.
CPC ...
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.


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