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Diterpene derivative as well as preparation method, pharmaceutical composition and application thereof

A technology of derivatives and compositions, applied in the field of diterpene derivatives and their preparation, can solve problems such as hair loss and limited chemotherapeutic drugs

Pending Publication Date: 2022-01-28
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although chemotherapy drugs have greatly improved the therapeutic effect of malignant tumors and effectively controlled the spread and metastasis of cancer, the choice of chemotherapy drugs is very limited, and side effects such as nausea, vomiting, and hair loss will also occur

Method used

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  • Diterpene derivative as well as preparation method, pharmaceutical composition and application thereof
  • Diterpene derivative as well as preparation method, pharmaceutical composition and application thereof
  • Diterpene derivative as well as preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of diterpene derivatives

[0020] (1) Preparation of compound 3:

[0021] The structure of compound 3 is as follows:

[0022] Its preparation process is as follows:

[0023] To a solution of pleuromutilin (compound 1, 7.00 g, 22.1 mmol) in ethanol (50 mL) and water (32 mL) was added 50% aqueous sodium hydroxide solution (3.70 mL) at room temperature. After stirring at 65°C for 1 hour, the reaction mixture was cooled to room temperature and filtered, the filtrate was acidified to pH=2 with 1N hydrochloric acid, then diluted with ethyl acetate (200 mL); the organic phase was separated and the aqueous phase was washed with ethyl acetate (3 × 200 mL) extraction; the combined organic phases were washed with saturated brine, dried over anhydrous sodium sulfate, concentrated in vacuo, and used directly in the next step as compound 2.

[0024] Compound 2 (200 mg, 0.63 mmol) was dissolved in EtOH (4 mL) and the solution was a colorless transparent liq...

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PUM

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Abstract

The invention discloses a diterpene derivative as well as a preparation method, a pharmaceutical composition and application thereof. The structure of the diterpene derivative is as shown in formula I, wherein R1 is phenyl, chain aliphatic hydrocarbon, cyclic aliphatic hydrocarbon or heteroatom-containing aromatic ring. The novel diterpenoid derivative is obtained, the preparation process is simple and easy to implement, and the diterpenoid derivative has a certain inhibition effect on proliferation of various tumor cells and is suitable for development of anti-tumor drugs.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and in particular relates to a diterpene derivative and its preparation method, pharmaceutical composition and application. Background technique [0002] Tumor refers to a new organism formed by the proliferation of local tissue cells under the action of various tumorigenic factors. Tumors, especially malignant tumors, are one of the most important factors that threaten human life and health. According to the latest statistics from the World Health Organization, about 10 million people will die of malignant tumors in 2020, becoming one of the diseases with the highest fatality rate in the world. There are 19.3 million new cases of malignant tumors globally in 2040, and it is expected to increase to 28.4 million cases in 2040, an increase of 47% compared with 2020. Among them, the number of cases in countries with medium and low population development indices has increased significantly, reaching ...

Claims

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Application Information

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IPC IPC(8): C07C49/743C07C45/64C07C49/753C07C319/20C07C323/22C07C51/373C07C59/90C07D295/116C07D307/46C07D213/50A61P35/00A61K31/122A61K31/19A61K31/5375A61K31/341A61K31/4406
CPCC07C45/64C07C49/743C07C49/753C07C319/20C07C323/22C07C51/373C07C59/90C07D295/116C07D307/46C07D213/50A61P35/00C07C2603/82C07C2601/14C07C2601/02C07C2601/08C07B2200/07
Inventor 杨诚曹胜王宁张坤杨光
Owner NANKAI UNIV
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