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Steroid derivative containing isatin unit as well as preparation method and application thereof
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A derivative, isatin technology, applied in the field of steroid derivatives containing isatin units and their preparation, can solve the problems of prolonging the survival time of cancer patients, unable to completely cure cancer, etc. Simple, easy to use, easy-to-obtain results
Active Publication Date: 2019-05-17
HUBEI BIOPESTICIDE ENG RES CENT
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Abstract
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Problems solved by technology
With the advancement of society's science and technology, human beings' understanding of cancer has gradually become clearer, and the methods, technologies and theories for the prevention and early diagnosis of certain cancers have also become more mature, but they cannot completely cure cancer, and can only prolong the life of cancer in a very limited way. patient survival time
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Embodiment 1
[0026] The structure of part of the steroid derivative containing isatin unit of the present invention is one of the specific compounds listed below, but is not limited to the structure listed in this embodiment:
[0027]
[0028]
Embodiment 2
[0030] Preparation of the compound numbered as I1 in embodiment 1
[0031] Its reaction formula is:
[0032]
[0033] Its preparation method comprises the following steps:
[0034] 1) With 1mmol of epiandrosterone (compound 1) and 5mmol of hydrazine hydrate (NH 2 NH 2 ·H 2 O) as the starting material, dehydration reaction was carried out in absolute ethanol (10mL) to prepare intermediate 2 (R configuration), the reaction temperature was 25-30°C, and the reaction time was 20-22h;
[0035] 2) The intermediate 2 (1 mmol) was condensed with isatin 3a (1.2 mmol) in methanol (10 mL) to obtain the target compound I1. The reaction temperature was 40-45° C. and the reaction time was 12 h.
[0038] Preparation of the compound numbered as I2 in embodiment 1
[0039] Its reaction formula is:
[0040]
[0041] Its preparation method comprises the following steps:
[0042] 1) With 1mmol of epiandrosterone (compound 1, R configuration) and 5mmol of hydrazine hydrate (NH 2 NH 2 ·H 2 O) is the starting material, and the intermediate 2 (R configuration) is prepared by dehydration reaction in anhydrousmethanol (10mL), the reaction temperature is 25~30°C, and the reaction time is 21~22h;
[0043] 2) The intermediate 2 (1 mmol) was condensed with 5-fluoroisatin 3b (1 mmol) in 15 mL of ethanol to obtain the target compound I2. The reaction temperature was 40-45° C. and the reaction time was 10 h.
[0044] Spectral data of target compound I2: 1 H NMR (600MHz, DMSO-d 6 ):δ=10.82(s,1H),7.56(dd,J=8.4,2.7Hz,1H),7.27-7.23(m,1H),6.88(dd,J=8.6,4.3Hz,1H),4.44( d,J=4.7Hz,1H),3.41-3.33(m,1H), 2.45(dd,J=19.4,8.6Hz,1H),2.37-2.26(m,1H),2.02(d,J=12.2Hz , 1H),1.81-1.74(m,1H),1.74...
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Abstract
The invention provides a steroid derivative containing an isatin unit as well as a preparation method and application thereof. The structure formula of the steroid derivative containing the isatin unit is as shown in the formula I (the formula is shown in the description). The preparation method of the compound comprises the steps that (1) a compound epiandrosterone or androsterone serves as an initial raw material to make dehydration reaction with hydrazine hydrate to obtain an intermediate; (2) the intermediate makes condensation reaction with substituation isatin in a solvent, so that a first kind of target compound with R1 being H is obtained; and (3) the first kind of target compound with R1 being H makes esterification reaction with chloride with the structure formula being R1Cl in asolvent, so that a second kind of target compound with R1 being CH3CO, CH3CH2CO, CH3SO2 or PhCO is obtained. The compound can serve as a substite product used for preparing active components of novelanticancer drugs.
Description
technical field [0001] The invention belongs to the technical field of organic synthesis and medicinal chemistry, and specifically relates to a steroid derivative containing isatin unit and its preparation method and application. Background technique [0002] Human health problems are an important field of life science research, and malignant tumors have become common and frequently-occurring diseases that seriously threaten human health, and are one of the major public health problems that people talk about. At present, the treatment methods for various cancers mainly include surgery, radiation therapy, drug therapy, photothermal therapy, photodynamic therapy, gene therapy and immunotherapy, etc., but drug therapy is still the main method. Most common solid tumors such as lungcancer, liver cancer, colon cancer, and pancreatic cancer still lack effective drugs, and many anti-tumor drugs have developed drug resistance during clinical application. Therefore, the research and ...
Claims
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