METHOD FOR PREPARING 1-(4-METHANESULFONYL-2-TRIFLUOROMETHYLBENZYL)-2-METHYL-1H-PYRROLO[2,3-B]PYRIDINE-3-YL-ACETIC ACID Russian patent published in 2021 - IPC C07D471/04 

Abstract RU 2756507 C2

FIELD: chemistry.

SUBSTANCE: invention relates to methods for producing 1-(4-methanesulfonyl-2-trifluoromethylbenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl-acetic acid (Compound A). The first producing method consists in the interaction of a compound of the formula C9 with dimethyl ether of diazomalonic acid (DMDA) in the presence of a catalyst and an organic solvent to form a compound of the formula C10. Then, a reaction of the compound of the formula C10 with a strong base/acid is carried out to obtain the Compound A. The second synthesis method includes a reaction of the compound of the formula C9 with halogen to form a compound of the formula C11. The resulting compound of the formula C11 is subjected to interaction with dimethylmaleate to form the compound of the formula C10, which is converted into the Compound A by the above-mentioned method.

EFFECT: methods consist of a smaller number of stages, allow one to achieve higher yield of the product and have higher selectivity for the Compound A.

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18 cl, 1 dwg, 37 ex

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RU 2 756 507 C2

Authors

Gallou, Fabrice

Lustenberger, Philipp

Mathes, Christian

Pan, Qiangbiao

Zou, Benli

Dates

2021-10-01Published

2018-03-29Filed