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. 09, 2014

Filed:

Jul. 05, 2011
Applicants:

Ronald Hage, Leiden, NL;

Jean Hypolites Koek, Vlaardingen, NL;

Stephen William Russell, Rhoon, NL;

Lodewijk Van Der Wolf, Vlaardingen, NL;

Jianrong Zhang, Shanghai, CN;

Wei Zhao, Shanghai, CN;

Xiaohong Wang, Shanghai, CN;

Inventors:

Ronald Hage, Leiden, NL;

Jean Hypolites Koek, Vlaardingen, NL;

Stephen William Russell, Rhoon, NL;

Lodewijk Van der Wolf, Vlaardingen, NL;

Jianrong Zhang, Shanghai, CN;

Wei Zhao, Shanghai, CN;

Xiaohong Wang, Shanghai, CN;

Assignee:

Catexel Limited, London, GB;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D 255/02 (2006.01); C07D 403/06 (2006.01);
U.S. Cl.
CPC ...
C07D 255/02 (2013.01); C07D 403/06 (2013.01);
Abstract

The present invention provides improved processes for the synthesis of 1,4-ditosyl-1,4,7-triazacyclonone, comprising deprotecting a compound of formula (C): wherein P is tosylate or arylsulfonate, with an acidic medium to form 1,2-bis(1,4,7-triazacyclonon-1-yl)-ethane; and subsequently adding formaldehyde and formic acid to the acidic medium to form 1,2-bis-(4,7-dimethyl-1,4,7-triazacyclonon-1-yl)-ethane (Me-DTNE). The syntheses of intermediates are also disclosed.


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