METHOD FOR PRODUCTION OF TYROSINE KINASE INHIBITOR AND ITS INTERMEDIATE COMPOUND Russian patent published in 2022 - IPC C07D209/48 C07D213/30 C07D215/54 C07D401/12 C07D401/14 C07D407/14 C07D495/04 

Abstract RU 2777675 C2

FIELD: biotechnology.

SUBSTANCE: invention relates to a method for the production of a compound represented by the formula II, which can be used in a method for the production of an effective tyrosine kinase inhibitor and its intermediate compounds. The method includes a stage of a reaction of a compound represented by the formula III with phosphorous oxychloride in the presence of a catalyst. The catalyst includes catalyst A, while catalyst A is phosphoric acid. In the specified formulas, R1 is phthalimido; R2 is selected from a group consisting of C1-6alkoxy; each of R3 is independently selected from a group consisting of halogen; R4 is characterized by the following structure: ; T is -O(CH2)r-; L is selected from a group consisting of 6-element heteroaryl containing 1 heteroatom selected from N; n is equal to 0, 1, 2, 3 or 4; r is equal to 1 or 2. The invention also relates to a method for the production of a compound represented by the formula II' and options of a method for the production of a compound represented by the formula I.

EFFECT: proposed method is characterized by high yield, good product purity and mild reaction conditions.

20 cl, 4 ex

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RU 2 777 675 C2

Authors

Feng, Guobing

Cao, Yongxing

Zhang, Peng

Qiu, Zhenjun

Zhang, Long

Dates

2022-08-09Published

2018-10-17Filed