SYNTHESIS METHODS OF AMATOXIN STRUCTURAL BLOCK AND AMATOXINS Russian patent published in 2017 - IPC C07C227/16 C07C229/22 C07D207/16 C07K7/52 

FIELD: chemistry.

SUBSTANCE: invention relates to a synthesis method γ,δ-dihydroxyisoleucine 1 or its hydroxy protected derivative (compound 6 ) as a synthone for compound 1, which can be used as structural blocks for the preparation of amatoxins. The method includes the step of methylating compound 3 or compound 3* containing the second benzyl protecting group at the nitrogen atom in place of the phenylfluorenyl group in compound 3 using methyl iodide in the presence of lithium bis (trimethylsilyl) amide (LHMDS). The invention also relates to a compound of structure 6, a kit for synthesizing amatoxins or their precursors, and a method for synthesizing amatoxin or a molecule that is a precursor thereof, using compound 6.

EFFECT: compound with high diastereomeric purity.

16 cl, 3 dwg, 7 ex