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Norcantharidin carboxylate tetrafluorobenzyl ester and synthesis method thereof

A technology of tetrafluorobenzyl methylcantharidin carboxylate and methylcantharidin carboxylic acid, which is applied in the field of medicine to achieve the effects of enhancing pharmacokinetic efficacy, readily available raw materials, and easy operation and implementation

Active Publication Date: 2022-08-09
ZUNYI MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] At present, there are few studies on the introduction of fluorine-containing groups into cantharidin. At the same time, in order to find anti-tumor drug candidates with better efficacy and less toxicity, and to expand the types of cantharidin anti-tumor drugs, we designed a fluorine-containing group The fluorine-containing derivatives of norcantharidin were synthesized, which laid the foundation for the subsequent screening of anticancer activity

Method used

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  • Norcantharidin carboxylate tetrafluorobenzyl ester and synthesis method thereof
  • Norcantharidin carboxylate tetrafluorobenzyl ester and synthesis method thereof
  • Norcantharidin carboxylate tetrafluorobenzyl ester and synthesis method thereof

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Embodiment Construction

[0032] The following will further illustrate the present invention through specific examples, which are not intended to limit the protection scope of the present invention. On the premise of not departing from the concept of the present invention, those skilled in the art can make improvements or combinations to the parameters or conditions of the claims, and these improvements or combinations should also be regarded as the protection scope of the present invention. Therefore, the protection scope of the patent of the present invention should be subject to the appended claims.

[0033] Furan, maleic anhydride, 2,3,4,5-tetrafluorobenzyl alcohol, 2,3,4,6-tetrafluorobenzyl alcohol, 2,3,5,6-tetrafluorobenzene used in the present invention Methanol was from Saen Chemical Technology (Shanghai) Co., Ltd.; the solvent used was from Shanghai Titan Technology Co., Ltd. Unless otherwise specified, all reagents used are chemically pure.

[0034] The synthetic method of the aforementione...

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Abstract

Norcantharidin carboxylate tetrafluorobenzyl ester and synthesis method thereof, its structural formula is shown in formula I, and the specific structure of norcantharidin carboxylate tetrafluorobenzyl ester shown in formula I includes: the molecular structure of the compound of the present invention introduces The carboxyl group improves water solubility and stability; due to the introduction of fluorine-containing groups, the physical properties, chemical properties and biological activities of the parent molecule can be significantly changed, thereby enhancing the pharmacokinetic efficacy. In addition, the raw materials of the synthesis method of the present invention are readily available, and the operation is very easy to implement.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a class of norcantharidin carboxylate tetrafluorobenzyl ester and a synthesis method thereof. Background technique [0002] Cantharidin (CA) is an anti-cancer substance extracted from Cantharidaceae, an insect of the family Corianaceae. It has good curative effect on liver cancer, ovarian cancer, esophageal cancer, etc., especially it has a special inhibitory effect on primary liver cancer. However, due to the severe toxicity of cantharidin, it can seriously stimulate the human urinary system and digestive system, and it has certain limitations in its clinical application. The synthetic cantharidin derivative norcantharidin (NCTD) has the same configuration as cantharidin, but the 2 and 3 methyl groups are replaced by hydrogen, and the toxic and side effects are significantly reduced. It can not only stimulate the bone marrow but also increase white blood cells. How...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/08C07D493/18A61P35/00
CPCC07D493/08C07D493/18A61P35/00
Inventor 李晓飞贺春阳贾佳王乐张建永晏容刘云
Owner ZUNYI MEDICAL UNIVERSITY
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