Process for manufacturing adamantane derivatives with high yield
AssigneeMERZ PHARMA GmbH & CO. KGaA
InventorsMarkus-Rene Gold, Herbert Koller, Michael Pyerin
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Abstract
The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine: substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.
Claims13
A process for the amidation of a substituted 1-bromo-adamantane comprising:
- step (0), wherein a substituted adamantane is reacted with an excess of bromine, wherein the reaction temperature in step (0) is between 50 to 100° C., to obtain a 1-bromo-adamantane and step (i), wherein the substituted 1-bromo-adamantane is reacted with an amide or urea and/or derivatives thereof to produce an amidation product, wherein the substituted 1-bromo-adamantane is used in the form of a mixture with bromine as obtained in step (0), and wherein, in step (0), a bromine:
- substituted adamantane molar ratio of from [2.8:1] to [3.5:1] is employed.
Dependencies are inferred from the claim text.