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Application of composition of Salviskinone A derivatives in drugs for increasing leukocytes

A technology for increasing white blood cells and compositions, which is applied in the field of preparation and compositions, and can solve problems such as low safety and high toxicity of white blood cells

Inactive Publication Date: 2016-10-12
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of leukopenia have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity

Method used

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  • Application of composition of Salviskinone A derivatives in drugs for increasing leukocytes
  • Application of composition of Salviskinone A derivatives in drugs for increasing leukocytes
  • Application of composition of Salviskinone A derivatives in drugs for increasing leukocytes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound Salviskinone A

[0011] The preparation method of the compound Salviskinone A (I) refers to the method published by Ayumi Ohsaki et al. (Ayumi Ohsaki et al., 2011. Salviskinone A, a diterpene with a new skeleton from Salviaprzewalskii. Tetrahedron Letters 52 (2011) 1375-1377).

[0012]

Embodiment 2

[0013] The synthesis of the O-bromoethyl derivative (II) of embodiment 2Salviskinone A

[0014] Compound I (312 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 12 h. After 12 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine four times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (327mg, 78%...

Embodiment 3

[0019] The synthesis of the O-(benzimidazolyl) ethyl derivative (III) of embodiment 3Salviskinone A

[0020] Compound II (209mg, 0.5mmol) was dissolved in 20mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and benzimidazole (1180mg, 10mmol) were added thereto, and the mixture was heated to reflux for 5h . After the reaction was completed, the reaction solution was poured into ice water, extracted three times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.5, v / v), and the concentrated brown elution band was collected and concentrated to give compound III as a brown solid (215 m...

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Abstract

The invention discloses an application of a composition of Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives in drugs for increasing leukocytes, relates to the fields of organic synthesis and medicinal chemistry, and particularly relates to the composition of the Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives, and a preparation method and the application thereof in preparation of the drugs for increasing the leukocytes. Provided are the composition of the Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives and the preparation method thereof. Pharmacological experiments indicate that the composition has an effect of increasing the leukocytes, and has the value for development of the drugs for increasing the leukocytes.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Leukopenia is a disease caused by unknown reasons and secondary to other diseases, which can be divided into two categories: primary and secondary. The primary cause is unknown; the secondary cause is believed to be caused by acute infection, physical and chemical factors, blood system diseases, diseases with splenomegaly, connective tissue diseases, allergic diseases, genetic diseases, etc., acquired or Unexplained neutropenia, etc. [0003] The existing drugs for the treatment of leukopenia have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity. [00...

Claims

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Application Information

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IPC IPC(8): A61K31/4164A61K31/145C07D235/04C07C323/25C07C319/14A61P7/00
CPCA61K31/145A61K31/4164C07C319/14C07C323/25C07D235/04A61K2300/00
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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