NOVEL METHODS OF PRODUCING PROPANE-1-SULPHONIC ACID {3-[5-(4-CHLORO-PHENYL)-1H-PYRROLO[2,3-b]PYRIDINE-3-CARBONYL]-2,4-DIFLUORO-PHENYL}-AMIDE Russian patent published in 2016 - IPC C07D471/04 C07D213/73 C07D213/74 C07D213/75 C07F5/02 C07F7/08 

Abstract RU 2575478 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound of formula 1, , which includes a Suzuki-Miyaura reaction, followed by Friedel-Crafts acylation, where a compound of formula 2 reacts in the presence of a palladium catalyst, a base and a compound of formula 3 (1st Suzuki-Miyaura reaction) to obtain a compound of formula 4 , the compound of formula 4 further reacts in the presence of a halogenating agent to obtain a compound of formula 5 , where X is I (5a) or Br (5b); and the compound of formula 5 further reacts in the presence of either a compound of formula (D) , or a compound of formula 7 (Sonogashira reaction), to obtain a compound of formula 8 , which further reacts in the presence of a compound of formula 9 and under Friedel-Crafts acylation conditions to obtain a compound of formula 1, where all R1, R2, R3 and R4 represent a methyl, or together with carbon atoms with which they are bonded form a phenyl ring; and R5 is -(C1-C6)alkyl.

EFFECT: novel method of producing a compound of formula 1 with high output.

4 cl, 9 ex

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RU 2 575 478 C2

Authors

Bramstid Kori Dzhejms

Moorlag Khendrik

Radinov Romen Nikolaev

Zhehn' I

Val'Dmajer Pius

Dates

2016-02-20Published

2011-07-18Filed