METHOD OF PRODUCING 5-HYDROXYALKYL-SUBSTITUTED DERIVATIVES OF 1-PHENYL-1,2,4-TRIAZOLE Russian patent published in 2021 - IPC C07D403/06 A61K31/4196 

Abstract RU 2742885 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound of formula (I), comprising steps of [C] and [D], wherein [C] a compound of general formula (XI), in which R2 denotes alkyl with 1–4 carbon atoms, is reacted one after another at the first step [C-1] in the presence of a base with an acid chloride of general formula (XII), where PG denotes a protective group, and obtained intermediate product is then reacted at next step [C-2] in presence of base with phenylhydrazine compound of general formula (XIII), wherein R1A and R1B are independently selected from a group consisting of hydrogen, fluorine, chlorine, methyl, monofluoromethyl, difluoromethyl, trifluoromethyl, ethyl, methoxy, difluoromethoxy and trifluoromethoxy, to obtain 1,2,4-triazolyl compound of general formula (XIV), in which the residues PG, R1A and R1B have the values given above, and at the next step [D] by removing the protective group PG is converted to a compound of general formula (I). Invention also relates to a compound of general formula (X), to a compound of general formula (XI).

,

EFFECT: novel method of producing a compound of formula (I) with high output, suitable for synthesis on an industrial scale.

12 cl, 1 dwg, 1 tbl, 23 ex

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RU 2 742 885 C2

Authors

Shirmer, Khajko

Rubenbauer, Filipp

Milittser, Khans-Kristian

Kollin-Krepelin, Mari-Pirre

Zyussmajer, Frank

Gerike, Kersten, Mattias

Nojbauer, Tomas

Fyurstner, Shantal

Dates

2021-02-11Published

2017-05-02Filed