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Compound for inhibiting KRASG12C mutant protein, preparation method and application thereof

A compound, unsaturated technology, used in medical preparations containing active ingredients, organic chemistry, drug combinations, etc., can solve problems such as far unmet drug needs

Inactive Publication Date: 2021-02-23
SUZHOU VINTAGENCE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, there is a potentially huge unmet drug need in this area

Method used

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  • Compound for inhibiting KRASG12C mutant protein, preparation method and application thereof
  • Compound for inhibiting KRASG12C mutant protein, preparation method and application thereof
  • Compound for inhibiting KRASG12C mutant protein, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Embodiment 1: the preparation of compound 1

[0104]

[0105] First prepare piperazine intermediate 1-5 according to the following route.

[0106]

[0107] Step 1: Synthesis of Intermediate 1-2

[0108] Compound 1-1 (4g, 18.5mmol) was dissolved in ethyl acetate (70ml), water (35ml), sodium bicarbonate solid (4.66g, 55.5mmol), benzyloxycarbonyl chloride (3.42ml, 24mmol) were added, Stir at room temperature for 2 hours. After the reaction, the organic phase was separated, washed with water (100ml*2), dried, concentrated, column chromatography (petroleum ether: ethyl acetate = 10:1 ~ 5:1) to obtain intermediate 1-2 (6.83g , colorless liquid).

[0109] Step 2: Synthesis of Intermediates 1-3

[0110] Compound 1-2 (6.83g, 19.5mmol), triethylamine (3.26ml, 23.4mmol) were dissolved in dichloromethane (60ml), p-toluenesulfonyl chloride (4.1g, 21.45mmol) was added dropwise, at room temperature Stir overnight. After the reaction was completed, it was concentrated and s...

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Abstract

The present invention discloses a compound represented by the following formula (I), and an isomer or a pharmaceutically acceptable salt thereof. The compound can be used for inhibiting KRASG12C mutant protein and treating related cancers.

Description

technical field [0001] The present invention relates to the field of drug synthesis, in particular to a compound that can be used to inhibit KRASG12C mutant protein, its preparation method and application. Background technique [0002] RAS mutations are frequently observed in malignancies and support various hallmarks of cancer, including genomic instability, cell proliferation, inhibition of apoptosis, reprogramming of metabolism, alteration of microenvironment, evasion of immune response and promotion of metastasis . Consistent with its pervasive effects on cancer cell function, regression of oncogenic KRAS in many established tumor models resulted in tumor regression. Therefore, RAS is a potentially very effective target for cancer therapy. RAS mutations appear to have multiple functional classes, and strategies for each functional class may be required. [0003] Among RAS family members, oncogenic mutations were most commonly found in KRAS (85%), while NRAS (12%) and ...

Claims

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Application Information

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IPC IPC(8): C07D403/14C07D403/04C07D491/052A61K31/517A61K31/519A61K31/5377A61P35/00A61P35/02
CPCC07D403/14C07D403/04C07D491/052A61P35/00A61P35/02
Inventor 余尚海李本
Owner SUZHOU VINTAGENCE PHARM CO LTD
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