NOVEL METHODS OF PRODUCING BARUSIBAN AND INTERMEDIATE COMPOUNDS THEREOF Russian patent published in 2020 - IPC C07K7/06 C07K1/04 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to novel solid-phase methods for peptide synthesis of analogues which exhibit oxytocin antagonist activity, especially barusiban and intermediate compounds thereof. In particular, the present invention relates to a solid-phase method of producing a compound having formula c[AA₁-AA₆]-AA₇-ol, where AA₁ is propionic acid, AA₂ preferably represents D-Trp, AA₃ represents Ile, AA₄ preferably represents AlloIle, AA₅ represents Asn, AA₆ is Hcy, and AA₇ preferably is N-Me-Orn-ol, or its pharmaceutically acceptable salt or solvate.

EFFECT: method demonstrates better reliability and is well adapted to obtain proper purity and output, which makes it suitable for large-scale production.

15 cl, 11 dwg, 5 tbl, 5 ex