Heteroaryl amide compound and preparation method, pharmaceutical composition and application thereof
A compound and solvate technology, applied in the field of medicinal chemistry, can solve the problem that tumor driver mutation genes are difficult to become therapeutic targets
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[0159] In another aspect, the present invention also provides a method for preparing the compound described in any of the above technical schemes, comprising the following steps:
[0160]
[0161] Reaction conditions: (a) (triethylamine, diisopropylethylamine, etc.) amide condensation reaction under alkaline conditions;
[0162]
[0163] Reaction conditions: (a) amide condensation reaction under basic conditions (triethylamine, diisopropylethylamine, etc.).
[0164] On the other hand, the present invention also provides the compound described in any of the above-mentioned technical schemes, its stereoisomer, its prodrug, or its pharmaceutically acceptable salt or pharmaceutically acceptable solvate and the compound containing the compound Use of drug combinations in drugs for treating tumors, wherein the tumors include but not limited to: gastric cancer, liver cancer, hematological tumors, osteosarcoma, prostate cancer, breast cancer, and lung cancer.
[0165] Experimen...
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[0189] The implementation of the present invention will be described in detail below through specific examples, but they should not be construed as limiting the present invention in any case.
[0190]
[0191] Wherein, the synthetic general formula of compound I:
[0192]
[0193] method one:
[0194]
[0195] Preparation of compound I:
[0196] method 1:
[0197] Compound 1 (0.2 mmol) was dissolved in N,N-dimethylformamide, HATU (0.3 mmol) and DIEA (0.8 mmol) were added, and compound 3 (0.2 mmol) was added under stirring at room temperature. React overnight at room temperature. Water / ethyl acetate extraction (3 x 15 mL), the organic phase was washed with saturated sodium chloride solution and dried over anhydrous sodium sulfate. Concentration and silica gel column chromatography (dichloromethane / methanol) gave compound I.
[0198] Method 2:
[0199] Compound 1 (0.2 mmol) was dissolved in N,N-dimethylformamide, HATU (0.3 mmol) and DIEA (0.8 mmol) were added, and...
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