PROCESS FOR THE DEPROTECTION OF A CARBAPENEM BY HETEROGENEOUS CATALYTIC HYDROGENATION WITH HYDROGEN IN THE PRESENCE OF AN ORGANIC AMINE

• Main Authors: WEIDLICH, Stephan, JANTKE, Ralf, GRÜNEWALD, Elena
• Format: Patent
• Language: English; French; German
• Published: 17.01.2018
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

Verfahren zur Herstellung eines Carbapenems oder dessen Vorstufe (I) durch Abspaltung einer oder mehrerer Schutzgruppen einer Substanz (II). enthaltend die Schritte: a) Hydrierung mit Wasserstoff eines Reaktionsgemisches (1) enthaltend die Substanz (II), mindestens ein organisches Lösungsmittel und mindestens ein aromatisches Amin in Gegenwart eines heterogenen Hydrierkatalysators unter Bildung eines Produktgemisches (1), b) Abtrennung des heterogenen Katalysators aus dem Produktgemisch (1) unter Bildung eines Produktgemisches (2), c) Hinzufügen von Wasser zum Produktgemisch (2), wobei das Gewichtsverhältnis von zugegebenem Wasser zum Produktgemisch (2) von 0,1 bis 10 ist, d) Thermische Behandlung des Produktgemisches (II) unter Bildung eines Produktgemisches (3) enthaltend Substanz (I). 201600080 17 Process for preparing a carbapenem Abstract Process for preparing a carbapenem or precursors thereof (I) by cleaving one or more protecting groups of a substance (II) 5 comprising the steps of: a) hydrogenating with hydrogen a reaction mixture (1) comprising the substance (II), at least 10 one organic solvent and at least one aromatic amine in the presence of a heterogeneous hydrogenation catalyst to form a product mixture (1), b) removing the heterogeneous catalyst from the product mixture (1) to form a product mixture (2), c) adding water to the product mixture (2), wherein the ratio by weight of water added to the 15 product mixture (2) is from 0.1 to 10, d) thermal treatment of the product mixture (2) to form a product mixture (3) comprising substance (I).