METHODS FOR OBTAINING BENZODIAZEPINE DERIVATIVES Russian patent published in 2023 - IPC C07D243/24 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a process for the preparation of a compound of formula (Ia), wherein the said process comprises (a) reacting a compound of formula (VII), where R₇ is selected from the group consisting of hydrogen, C₁-C₈-alkyl, C₂-C₈- alkenyl, C₂-C₈-alkynyl, C₃-C₈-cycloalkyl, C₃-C₈-cycloalkenyl, 3-8-membered heterocyclic fragment, aryl and heteroaryl; and X is chloro; with a compound of formula (VII-X), where PG is hydrogen; to form a compound of formula (VIII-d); (b) reacting a compound of formula (VIII) with morpholine to form a compound of formula (Xd); c) reaction of a compound of formula (IV) with 1.1'-carbonyldiimidazole or nitrophenylchloroformate to give a compound of formula (III) wherein R₅ is 1-imidazolyl or nitrophenyl-O-; d) isolation and purification of the compound of formula (III); (e) reacting a compound of formula (III) with a compound of formula (Xd), said reaction being carried out at a temperature of from about 10 to 50°C for 6 to 48 hours and at a concentration of the compound of formula (III) from about 1 M to 3 M and a molar ratio of compound of formula (III) and compound of formula (Xd) 1:1, to obtain a compound of formula (Va), and (f) reacting a compound of formula (Va) with a cyclization reagent to form a compound of formula (I-a).

EFFECT: method for obtaining biologically active molecules, respiratory syncytial virus (RSV) inhibitors.

14 cl, 4 ex

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