A kind of benzimidazole azetidinone derivative and its application in antitumor drug
A technology for azetidinone and antitumor drugs, which is applied to benzimidazole azetidinone derivatives and their application fields in antitumor drugs, can solve problems such as unreported new structure compounds, and achieve cost The effect of low, simple operation process and short synthesis route
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Embodiment 1
[0042] where R 1 is an alkyl group, R 2 For the hydrogen atom, that is, the synthesis of 2-(1H-benzimidazol-2-yl)-1-(2-bromobenzyl)-4-oxoazetidine-2-carboxylic acid ethyl ester, specific steps as follows:
[0043] In a 10 mL microwave reaction tube, ethyl glyoxylate (1.5 mmol) and 2-bromobenzylamine (1.0 mmol) were first dissolved in 2.0 mL of methanol solution, and then bromoacetic acid (1.0 mol) and isocyanide (1.0 mmol) were added in this solution successively, and the reaction solution was stirred overnight at room temperature, and then the isocyanate was detected by thin-layer chromatography. If there was no remaining isocyanine raw material, the solution was dried with nitrogen, and then Dissolve it with 5.0 ml of dimethylformamide (DMF), then add diisopropylamine (DIPA) (2.0 mmol), and react in a microwave oven at 90° C. for 10 minutes. The solution was diluted with ethyl acetate (15 mL), and washed three times with saturated brine, 20 mL each time. After the organi...
Embodiment 2
[0046] where R 1 is an alkyl group, R 2For the synthesis of hydrogen atom, i.e. 2-(1H-benzimidazol-2-yl)-1-benzyl-4-oxoazetidine-2-carboxylic acid ethyl ester, the specific steps are as follows:
[0047] In a 10 mL microwave reaction tube, ethyl glyoxylate (1.5 mmol) and benzylamine (1.0 mmol) were first dissolved in 2.0 mL of methanol solution, and then bromoacetic acid (1.0 mmol) and Isocyanides (1.0 mmol) were sequentially added to the solution, and the reaction solution was stirred overnight at room temperature, and then the isocyanides were detected by thin-layer chromatography. If there was no remaining isocyanide raw material, the solution was dried with nitrogen, and then 5.0 A milliliter of dimethylformamide (DMF) was dissolved, and then diisopropylamine (DIPA) (2.0 mmol) was added, and reacted in a microwave oven at 90° C. for 10 minutes. The solution was diluted with ethyl acetate (15 mL), and washed three times with saturated brine, 20 mL each time. After the or...
Embodiment 3
[0050] where R 1 is an alkyl group, R 2 For the hydrogen atom, that is, the synthesis of 2-(1H-benzimidazol-2-yl)-1-(3-fluorobenzyl)-4-oxoazetidine-2-carboxylic acid ethyl ester, specific steps as follows:
[0051] In a 10 mL microwave reaction tube, ethyl glyoxylate (1.5 mmol) and 3-fluorobenzylamine (1.0 mmol) were first dissolved in 2.0 mL of methanol solution, and then bromoacetic acid (1.0 mol) and isocyanide (1.0 mmol) were added in this solution successively, and the reaction solution was stirred overnight at room temperature, and then the isocyanate was detected by thin-layer chromatography. If there was no remaining isocyanine raw material, the solution was dried with nitrogen, and then Dissolve it with 5.0 ml of dimethylformamide (DMF), then add diisopropylamine (DIPA) (2.0 mmol), and react in a microwave oven at 90° C. for 10 minutes. The solution was diluted with ethyl acetate (15 mL), and washed three times with saturated brine, 20 mL each time. After the orga...
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