BIOORTHOGONAL COMPOUNDS COMPRISING A PROPARGYL GROUP FOR TREATING CANCER

A method of preparing an active agent or a salt thereof from a pro-drug first compound (1) comprising a propargyl group connected to an oxygen that is directly or indirectly connected to the active agent is provided, wherein the bond between the propargyl group and the oxygen is cleaved by reacting...

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Bibliographic Details
Main Authors RUBIO-RUIZ, Belen, ADAM, Catherine, UNCITI-BROCETA, Asier, BRAY, Thomas L, PEREZ-LOPEZ, Ana M
Format Patent
LanguageEnglish
French
German
Published 27.03.2019
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
DERIVATIVES THEREOF
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SUGARS
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Summary:A method of preparing an active agent or a salt thereof from a pro-drug first compound (1) comprising a propargyl group connected to an oxygen that is directly or indirectly connected to the active agent is provided, wherein the bond between the propargyl group and the oxygen is cleaved by reacting the first compound with palladium or gold, thereby releasing the active agent. Prodrug compositions suitable for use in the method are also provided.
Bibliography:Application Number: EP20170730892