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Synthesis method of 2,8-diaryl(amino) Troger's base derivatives

A technology of amino chaogle base and chaogle base, which is applied in the field of synthesis of chaogle base derivatives, can solve the problem of lack of Kang liver cancer drugs

Active Publication Date: 2015-09-23
南京百鑫德诺生物科技有限公司
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Problems solved by technology

[0005] The purpose of the present invention is to provide a kind of synthetic method of 2,8-diaryl (amino) chaogel base derivative, introduce the segment that has physiological activity such as phenothiazine, carbazole into TB skeleton, hope to pass both Compounds with anti-liver cancer activity were screened out by the powerful combination of the company to solve the serious shortage of Kangkang liver cancer drugs

Method used

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  • Synthesis method of 2,8-diaryl(amino) Troger's base derivatives
  • Synthesis method of 2,8-diaryl(amino) Troger's base derivatives
  • Synthesis method of 2,8-diaryl(amino) Troger's base derivatives

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Embodiment 1

[0048] Embodiment 1: 2,8-diaryl (amino) Chaoger base derivatives of the present invention include: 2(8)-triarylpyridine (tripyridine) Chaoger base (TB) derivatives, 2,8 - diaryl Chaoger base (TB) derivatives and 2-aryl-8-amino Chaoger base (TB) derivatives;

[0049] 1. Synthesis method of 2(8)-triarylpyridine (tripyridine) Chaoger base derivative, substance of "2(,8)-triarylpyridine (tripyridine) Chaoger base (TB) derivative" The structure is as follows:

[0050]

[0051] (a) TFA, -15℃-0℃, 6d; (b) n-BuLi, trimethyl borate, -78℃-r.t.; (c) Pd(PPh 3 ) 4 , K 2 CO 3 ,toluene,110℃(THF,70℃)

[0052] The method comprises the steps of:

[0053] 1) Synthesis of compound 1a, i.e. 2,8-dibromochauger base:

[0054] Add 60mmol p-bromoaniline and 120mmol paraformaldehyde into a 250mL dry three-necked round-bottom flask at -15°C, slowly drop 120mL trifluoroacetic acid (TFA) into it with a constant pressure funnel under stirring, the solution turns maroon, after the addition is compl...

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Abstract

The invention discloses a synthesis method of 2,8-diaryl(amino) Troger's base derivatives, belonging to the synthesis method of the Troger's base derivatives. The 2,8-diaryl(amino) Troger's base derivatives comprise 2(8)-triarylpyridyl (tripyridyl) Troger's base (TB) derivative, 2,8-diaryl Troger's base (TB) derivative and 2-aryl-8-amino Troger's base (TB) derivative; the synthesis method adopts Suzuki reaction to respectively introduce triarylpyridyl, tripyridyl, phenyl, phenanthryl or anthryl fragment into the TB skeleton, and Ullmann reaction to introduce carbazole, diphenylamine or phenothiazine into the TB skeleton, to obtain the new 2,8-diaryl(amino) Troger's base (TB) derivatives. Four products with excellent human liver cancer HepG2 cell activity resistance are selected from all products with human liver cancer HepG2 cell activity resistance. The method introduces phenothiazine, carbazole and other fragments with physiological activities into the TB skeleton, to design and synthesize 2,8-diaryl(amino) Troger's base derivatives for the first time, so as to screen compounds with liver cancer activity resistance through the combination of both.

Description

technical field [0001] The invention relates to a synthesis method of Chaoger base derivatives, in particular to a synthesis method of 2,8-diaryl (amino) Chaoger base derivatives. Background technique [0002] Liver cancer is one of the most common malignant tumors. Current treatment methods include surgery, radiation therapy, and drug therapy. Surgical treatment can delay or even stop the proliferation of liver cancer cells, but it will cause serious secondary damage to the patient. Some patients died of wound infections after surgery to remove the cancerous lesions of their livers, as their bodies were already overwhelmed. Chemical drugs can reduce the patient's pain and prolong the survival time, so it is an ideal important means and treatment method. Therefore, in recent years, the research and development of new drugs against liver cancer has become a multi-disciplinary field of pharmacy, chemistry, pharmacology, and toxicology, which has important practical signific...

Claims

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Application Information

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IPC IPC(8): C07D487/08A61P35/00A61P1/16
CPCC07D487/08
Inventor 宛瑜邱峰黄树颖吴翚
Owner 南京百鑫德诺生物科技有限公司
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