Methods for synthesizing amatoxin building block and amatoxins
AssigneeHeidelberg Pharma GmbH
InventorsChristian Lutz, Christoph Mueller, Werner Simon
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Abstract
The invention relates to novel methods for synthesizing a synthon for γ,δ-dihydroxyisoleucine 1 (CAS No. 55399-94-5] as building block for the synthesis of amatoxins, and for novel methods for synthesizing amatoxins using such building block.
Claims19
A method for the synthesis of γ, δ-dihydroxyisoleucine 1, or of a synthon for compound 1, comprising the step of methylating compound 3 or 3*, wherein the 3* has a second benzyl group at the nitrogen atom instead of the phenyl fluorenyl group in compound 3, with methyl iodide in the presence of lithium bis(trimethylsilyl)amide (LHMDS):
A compound of structure 6:
A method for synthesizing an amatoxin, or precursor molecule therefore, comprising the step of (a) coupling compound 6 to hydroxyproline L to create compound G:
Dependencies are inferred from the claim text.