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:
Jan. 26, 2016

Filed:

Dec. 19, 2014
Applicant:

Boehringer Ingelheim International Gmbh, Ingelheim am Rhein, DE;

Inventors:

Juncheng Zheng, Shanghai, CN;

Da Deng, Shanghai, CN;

Guanghua Lv, Shanghai, CN;

Jun Yan, Shanghai, CN;

Joerg Brandenburg, Wiesbaden, DE;

Jutta Kroeber, Bingen, DE;

Ulrich Scholz, Bad Kreuznach, DE;

Assignee:

Boehringer Ingelheim International GmbH, Ingelheim am Rhein, DE;

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07C 227/00 (2006.01); C07D 405/00 (2006.01); C07C 221/00 (2006.01); C07D 405/04 (2006.01); C07C 227/18 (2006.01); C07C 227/16 (2006.01); C07C 227/10 (2006.01);
U.S. Cl.
CPC ...
C07D 405/04 (2013.01); C07C 221/00 (2013.01); C07C 227/10 (2013.01); C07C 227/16 (2013.01); C07C 227/18 (2013.01);
Abstract

The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein Rand Rindependently denote C-alkyl groups and Xdenotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.


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