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Structure, preparation method and application of isothiocyanate-type precursor compound

A technology of isothiocyanate and compounds, applied in organic chemistry, drug combination, antineoplastic drugs, etc., can solve the problem of non-existence of isothiocyanate, and achieve stable structure, low drug resistance, and small toxic and side effects Effect

Inactive Publication Date: 2016-11-23
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] But so far, no prodrugs of isothiocyanates exist and improvements in this area are expected

Method used

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  • Structure, preparation method and application of isothiocyanate-type precursor compound
  • Structure, preparation method and application of isothiocyanate-type precursor compound
  • Structure, preparation method and application of isothiocyanate-type precursor compound

Examples

Experimental program
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Embodiment Construction

[0047] The following examples can enable those skilled in the art to understand the present invention more fully, but do not limit the present invention in any way.

[0048] The general formulas of the active form (I) of the drug and its prodrug (II) are shown below:

[0049]

[0050] where R 1 for: C 4 -C 6 Alkyl, C 1 -C 4 Alkoxy, C 1 -C 6 Alkenyl, C 2 -C 10 Alkynyl, C 1 -C 4 Alkanoyl, C 1 -C 4 alkanoyloxy,

[0051] R 2 for:

[0052] R 3 For: Cl, Br, alkyl, C 1 -C 6 Alkenyl, C 2 -C 10 Alkynyl, C 1 -C 4 Alkanoyl, C 1 -C 4 Alkanoyloxy; R 4 For: H, OH, CF 3 or methoxy;

[0053] X is: O, S or NH; n=0,1,2.

[0054] The synthetic steps and maps of various compounds are described below. The synthesis process of dimethylamino-(phenyl-1H-tetrazolium) isothiocyanate conjugate (represented by compound 1) is as follows:

[0055]

[0056] Each step is described step by step below.

[0057] Synthesis of 2-[4-((1-phenyl-1H-tetrazol-5-yl)thio)butyl...

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Abstract

The invention provides a structure of an isothiocyanate-type precursor compound. The general formula of the compound is shown in the specification,wherein R1 refers to H3C-, CH3CH2-, CH3CH2CH2-, C4-C6 alkyl, C1-C4 alkoxy, C1-C6 alkenyl, C2-C10 alkynyl, C1-C4 alkyl-acyl, C1-C4 alkyl-acyloxy, or other groups as shown in the specification. R2 refers to one of the groups as shown in the specification. R3 refers to Cl, Br, alkyl, C1-C6 alkenyl, C2-C10 alkynyl, C1-C4 alkyl-acyl or C1-C4 alkyl-acyloxy. R4 refers to H, OH, CF3 or methoxyl. X refers to O, S or NH. N equals to 0, 1 or 2. The invention further provides a preparation method and application of the isothiocyanate-type precursor compound. The isothiocyanate-type precursor compound can release active compounds slowly, drug resistance is low, toxic and side effect is small, and the isothiocyanate-type precursor compound can be used for preventing or treating various cancers.

Description

technical field [0001] The present invention relates to the field of pharmaceutical compounds, more specifically, to the structure, preparation and application of isothiocyanate precursor compounds. Background technique [0002] During the research process, it was found that some pharmaceutical compounds are unstable in structure, and at the same time, they are not easy to store in air and normal temperature environment. However, these existing anticancer drugs are not easy to achieve effective drug concentration in the human body, and the action time is short, so they cannot fully exert the anticancer effect. Therefore, the study of anti-tumor drug sustained-release system has become the focus of tumor drug therapy. Slow-release drugs can enhance the targeting of tumor cells or tissues, while prolonging the drug release time, reducing the absorption rate, stabilizing the blood drug concentration, and reducing side effects . The present invention aims to find a prodrug wit...

Claims

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Application Information

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IPC IPC(8): C07D277/74C07C333/20C07D257/04A61P35/00A61P35/02
CPCC07C333/20C07D257/04C07D277/74
Inventor 饶子和杨诚陈悦白翠改褚晓倩孙涛郭宇江银于建明管文豪董艳伟戴东方
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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