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Piperazine compound and application thereof

A compound, piperazine technology, applied in the field of piperazine compound and its application, can solve problems such as shock, achieve low production cost, simple preparation process, and excellent inhibitory activity effect

Pending Publication Date: 2021-11-26
上海药明康德新药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The new coronavirus pneumonia (COVID-19) caused by the new coronavirus (SARS-CoV-2) is an acute infectious pneumonia. Although most patients have a good prognosis, some severe cases may develop acute respiratory distress syndrome or sepsis Symptomatic shock, or even death. For COVID-19, isolation treatment, symptomatic and supportive treatment are mainly used, and there is no specific drug

Method used

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  • Piperazine compound and application thereof
  • Piperazine compound and application thereof
  • Piperazine compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 4-(4-acryloyl-2-methylpiperazin-1-yl)-N-((R)-1-(methylamino)-1-oxyylidene-3-phenylpropan-2-yl ) Synthesis of nicotinamide (I-1)

[0047]

[0048] Step 1. Synthesis of 4-(2-chloro-5-methoxycarbonyl-4-pyridyl)-3-methyl-piperazine-1-carboxylic acid tert-butyl ester (23)

[0049]

[0050] Add 20mL DMF solvent to the reaction flask, weigh compound 21 (4.00g, 19.4mmol) into the reaction flask, and then add K 2 CO 3 (8.05g, 58.3mmol), compound 22 (5.83g, 29.1mmol). The reaction was performed at 55° C., and whether the reaction was complete was checked by TLC. After the reaction, add H 2 O (10 mL) quenched the reaction. After the reaction was quenched, CH 2 Cl 2 (20mL×2) to extract, collect the organic phase solution, and use Na 2 SO 4 dry. Filter out Na 2 SO 4 Afterwards, the organic solvent was spin-dried. The product 23, (white liquid, 2.44 g, 6.44 mmol, 33.2% yield) was obtained by separation by column chromatography separation technique.

[0051] LC-MS:...

Embodiment 2

[0075] Research on the inhibitory activity of compounds on target proteins

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Abstract

The invention discloses a piperazine compound as shown in a formula I or a pharmaceutically acceptable salt, enantiomer, diastereoisomer or raceme thereof. The definition of each group in the formula is shown in the specification. In addition, the invention also discloses a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in preparation of drugs for inhibiting 3CL hydrolase (Mpro) of coronavirus.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a piperazine compound and its application. Background technique [0002] The new coronavirus pneumonia (COVID-19) caused by the new coronavirus (SARS-CoV-2) is an acute infectious pneumonia. Although most patients have a good prognosis, some severe cases may develop acute respiratory distress syndrome or sepsis Symptomatic shock, or even death, for COVID-19 is mainly isolated treatment, symptomatic and supportive treatment, and there is no specific medicine. At present, research work on anti-SARS-CoV-2 drugs is being actively carried out at home and abroad. The ideal antiviral drug can selectively interfere with a certain link in the virus replication cycle, thereby inhibiting its replication process, but does not affect the host cell. normal physiological function. [0003] 3CL hydrolase (M pro ) is highly conserved in all coronaviruses and plays an important role in mediat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04C07D401/14A61P31/14A61P11/00A61K31/496
CPCC07D401/04C07D401/14A61P31/14A61P11/00C07B2200/07
Inventor 李岳葛蕊潘舜杰何婧陈文华张琦安玉龙苏文姬蒯乐天吴阿亮
Owner 上海药明康德新药开发有限公司
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