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:
Apr. 13, 2021

Filed:

May. 02, 2018
Applicants:

Meda Pharma Gmbh & Co. KG, Homburg, DE;

Meda Ab, Solna, SE;

Inventors:

Borut Gabriel, Borovnica, SI;

Alja{hacek over (z)} Kajtna, Ljubljana, SI;

Ajna Lukic, Smarje-Sap, SI;

Dominic De Souza, Regau, AT;

Werner Hasselwander, Oberkirch, DE;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 498/18 (2006.01);
U.S. Cl.
CPC ...
C07D 498/18 (2013.01); C07B 2200/13 (2013.01);
Abstract

The present disclosure is directed to an improved process to convert crude ascomycin to purified pimecrolimus. Crude ascomycin is chlorinated with triphenylphosphine and N-chlorosuccinimide (NCS) to yield crude pimecrolimus, which is then purified further by HPLC and subsequent crystallization. The processes of the present disclosure enable the removal of close homologs of pimecrolimus by high-pressure liquid chromatography without prior purification of the ascomycin starting material. This improvement may make the conversion of ascomycin to pimecrolimus industrially applicable and less expensive.


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