METHOD FOR PRODUCTION OF BENZOTHIOPHENE-2-YLBORONATE Russian patent published in 2023 - IPC C07D333/54 C07D487/04 C07F5/02 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a method for the production of benzothiophene-2-ylboronate of the formula (VI). The method includes following stages: stage 5, at which a compound of the formula (VII) is subjected to a reaction by dissolution of the compound of the formula (VII) in an inert solvent, such as THF, and addition of an organometallic base, such as n-butyllithium solution, and trialkyl borate, such as triiso-propylborate, optionally in a solvent, such as THF, thus obtaining the compound of the formula (VI). At the same time, the specified compound of the formula (VII) is obtained at the following stage 4, at which a compound of the formula (X) is subjected to a reaction, optionally in the presence of an inert solvent, such as THF, with one or several reducing agents, such as a solution of sodium-bis(2-methoxy-ethoxy)-aluminum-dihydride, thus obtaining a compound of the formula (IX), and the compound of the formula (IX) is subjected to a reaction with aqueous HCl in the presence of a solvent, such as toluene, thus obtaining a compound of the formula (VIII). Then, the compound of the formula (VIII) is subjected to a reaction with one or several reducing agents, such as a solution of sodium-bis(2-methoxy-ethoxy)-aluminum-dihydride, thus obtaining the compound of the formula (VII). The use of a compound selected from a compound of the formula (VIII) and the formula (X) for the production of a compound of the formula (VI) is also proposed.

EFFECT: proposed method allows for provision of an efficient method for the production of benzothiophene-2-ylboronates of the formula (VI) with a high yield, which serve as a key component for the production of Rogaratinib with a high yield.

7 cl, 10 ex