METHOD OF PRODUCING {6-[(DIETHYLAMINO)METHYL]NAPHTHALEN-2-YL}METHYL[4-(HYDROXYCARBAMOYL)PHENYL]CARBAMATE HAVING HIGH PURITY Russian patent published in 2024 - IPC C07C269/06 C07C269/08 C07C271/28 A61K31/325 

Abstract RU 2826216 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and pharmaceutics, specifically to a method for synthesis of givinostat ({6-[(diethylamino)methyl]naphthalen-2-yl}methyl[4-(hydroxycarbamoyl)phenyl]carbamate), which exhibits activity in multiple myeloma and acute myelogenous leukaemia, and also functions as an anti-inflammatory agent. Method of producing givinostat and/or its pharmaceutically acceptable salts, having an amount of any single unidentified impurity equal to or less than 0.10%, involves two steps. First step is characterized by reacting a halogenating agent with a compound of formula (I) in an acid-insensitive aprotic dipolar solvent to obtain a compound of formula (II), where X is a halogen atom, preferably a chlorine atom. Step 2 consists in preparing a solution or suspension of the compound of formula (II) in an organic solvent and adding hydroxylamine thereto.

EFFECT: providing a method for obtaining a highly pure target product.

9 cl, 1 dwg, 1 tbl, 11 ex

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RU 2 826 216 C2

Authors

Turchetta, Stefano

Zenoni, Maurizio

Ullucci, Elio

Cocciolo, Stefania

Berardi, Giorgio

Maulucci, Nakia

Dates

2024-09-05Published

2020-03-05Filed