PROCESS FOR PRODUCING CGRP RECEPTOR ANTAGONISTS Russian patent published in 2018 - IPC C07D471/20 C07D213/61 C07D213/62 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, particularly to a process for producing a compound of formula I or a pharmaceutically acceptable salt thereof, comprising reacting a compound of formula F in an organic phase in the presence of a bis-quaternary cinchona alkaloid salt and an inorganic base in an aqueous phase, with the formation of a two-phase medium containing an aqueous phase and an organic phase, to obtain a compound of formula G, when E¹ is different from -C(O)-O-H, the substitution of E¹ with a carboxylic acid or conversion of E¹ into a carboxylic acid in a suitable chemical reaction to yield a compound of formula H, deprotection of the compound of formula H to yield a compound of formula C, optionally isolated as a salt, and linking the compound of formula C with a compound of formula B, optionally as a salt, under amide bonding conditions between an acid and an amine to yield a compound of formula I. Invention also relates to intermediates. I, F, G, H, C, B.

EFFECT: method has been developed for the preparation of piperidinone carboxamide indane and azainane derivatives that are antagonists of CGRP receptors suitable for the treatment of migraine using highly effective synthesis of spiro acids.

18 cl, 4 tbl, 10 ex