METHOD OF PRODUCING A NOVEL NITROGEN-CONTAINING COMPOUND OR A SALT THEREOF AND PRODUCING AN INTERMEDIATE THEREOF Russian patent published in 2020 - IPC C07D471/04 C07D255/02 C07D257/02 C07F1/08 C07F5/00 A61K31/4375 A61K31/555 

Abstract RU 2720989 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a method of producing a compound of formula [11], or a salt thereof, comprising: (1) a step for reacting a compound of formula [1] or a salt thereof:

where R1 represents a hydrogen atom or an amino protecting group which is selected from C1-6 alkoxycarbonyl group, a chromansulphonyl group substituted with C1-6 alkyl groups, or dihydrobenzofuransulphonyl group substituted with C1-6 alkyl groups; R2 represents C1-6 alkyl group; L1 is a group of formula [18a]

where R5a and R6a are a hydrogen atom and r1 is integer from 1 to 6; and L2 is a group of formula [18b]

where R5b and R6b are a hydrogen atom and r2 is integer from 1 to 6; with a compound of formula [3], or a salt thereof in the presence of a condensing agent

where L3 is a group of formula [18c]

where R5c and R6c represent a hydrogen atom and r3 is integer from 1 up to 6; A1 is any of groups of formulas [4] or [5]:

where * is a binding position; R7 are identical and represent C1-6 alkyl group; and m is integer from 1 to 3; to obtain a compound of formula [10], or a salt thereof:

and (2) a step for deprotection of a compound of formula [10], or a salt thereof in the presence of an acid, to obtain compound [11], in which A2 is any of groups of formulas [12] or [13]:

Invention also relates to a method of producing a metal complex, to a compound of formula [19], to a compound of formula [3], to a compound of formula [11], to a compound of formula [38], to complexes of compounds, structural formulas of compounds are given in the claim.

EFFECT: disclosed is a method of producing novel nitrogen-containing compounds of formula [11], which can be used for treating diseases associated with integrin.

17 cl, 6 dwg, 7 tbl, 27 ex

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RU 2 720 989 C2

Authors

Fukunaga, Hirofumi

Shinjo, Sachiko

Nakagawa, Daisuke

Sekine, Shinichiro

Yamakawa, Takayuki

Dates

2020-05-15Published

2016-03-25Filed