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Preparation and application of medium-ring-containing tetrahydrocarboline-tetrahydroisoquinoline compound

A compound, C1-C6 technology, applied in the field of medicine, can solve the problems of anti-cancer drug toxicity and side effects, achieve the effect of perfecting the structure-activity relationship, facilitating the development, and enriching the compound library

Pending Publication Date: 2021-10-12
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the drug resistance of cancer cells and the side effects of anticancer drugs, it is urgent to develop anticancer drugs with good curative effect and low side effects.

Method used

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  • Preparation and application of medium-ring-containing tetrahydrocarboline-tetrahydroisoquinoline compound
  • Preparation and application of medium-ring-containing tetrahydrocarboline-tetrahydroisoquinoline compound
  • Preparation and application of medium-ring-containing tetrahydrocarboline-tetrahydroisoquinoline compound

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Embodiment Construction

[0226] The following examples are given to describe the present invention in more detail, but the present invention is not limited to these examples.

[0227] Preparation of Compound 1-19

[0228] It can be prepared from the common precursor amine C by one-step acylation reaction, and the precursor amine C is prepared by multi-step reaction of tetrahydrocarboline intermediate A and carboxylic acid intermediate B. The preparation method of the carboxylic acid intermediate B can refer to the literature Liu, Z.Z.et al., Bioorg.Med.Chem.Lett.2006, 16, 1282.

[0229] 1. Preparation of tetrahydrocarboline intermediate A:

[0230]

[0231] a:SOCl 2 ,DCM,reflux; b:TMSCH 2 N 2 ,DCM; c:Silver benzoate,Na 2 CO 3 ,MeOH; d:DEA,DCM; e:BnOCH 2 CHO, TFA, CH 2 Cl 2 ; f:LiAlH 4 , THF; g: TBSCl, Imidazole, CH 2 Cl 2

[0232] Preparation of Intermediate A-1: ​​Dissolve 5g of Fmoc-L-tryptophan in 60mL of dichloromethane, cool in an ice bath to 0°C, slowly add 0.85mL of thionyl chlo...

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Abstract

The invention belongs to the technical field of medicines, and discloses preparation and application of a medium-ring-containing tetrahydrocarboline-tetrahydroisoquinoline compound. The invention specifically relates to a compound shown in a general formula I and pharmaceutically acceptable salts thereof, a preparation method of the compound, a pharmaceutical composition containing the compound shown in the general formula I, a preparation method of the pharmaceutical composition and application of the compound and the pharmaceutical composition in the anti-tumor aspect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a structural analogue of an anti-tumor marine natural product ecteinascidin and a pharmaceutically acceptable salt thereof, and an anti-tumor preparation containing the compound and a pharmaceutically acceptable salt thereof. Background technique [0002] Cancer is listed by the World Health Organization as one of the five deadly diseases in the world. According to the statistics of the World Health Organization, the number of people who will die of cancer worldwide will exceed 13.1 million by 2030. In my country, there is one cancer patient among every 65 people, and more than 4 million people are diagnosed with cancer every year. More than 10,000 people are diagnosed with cancer every day, and more than 5 people die of cancer every minute. The cancer mortality rate in China has increased by about 80% in the past 30 years, and cancer is currently the number one killer of people's...

Claims

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Application Information

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IPC IPC(8): C07D471/22A61P35/00A61P35/02A61K31/551
CPCC07D471/22A61P35/00A61P35/02
Inventor 刘站柱马艳涛潘璇贯宝和张广艳于瑞
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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