METHODS AND INTERMEDIATE COMPOUNDS FOR PRODUCING A PDE10 INHIBITOR Russian patent published in 2020 - IPC C07D413/10 C07D417/10 C07F1/02 C07F3/02 C07D307/40 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a method of producing a compound of formula (II), which includes converting boronic acid A1 to carbaldehyde B1 by activating boronic acid with an activating substance A2; converting carbaldehyde B1 into acetal C1 by acid catalysis with an orthoformate source; converting acetal C1 to nitrile D1 by catalysed cyanation with a metal catalyst and a cyanide source; hydrolysis of D1 with an acid to obtain carboxylic acid E1; converting carboxylic acid E1 into amide F1 with a base, a binder reagent and an amine source; converting amide F1 into a compound of formula (II) with an anionic coupling reagent having structure H1, where M is Mg; R, R² and R³ each independently represent C_(1-6)-alkyl; m equals 2; p equals 3; and, if necessary, converting the compound of formula (II) into a salt. Invention also relates to intermediate compounds, a compound of formula H1 and a method of production thereof, a method of producing a compound of formula (III), a special case of the compound of formula (II).

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EFFECT: technical result is a novel method of producing compounds (II) and (III) useful as a PDE10 inhibitor.

68 cl, 1 tbl, 8 ex