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Isoquinoline-3-formyl-RC-OBzl, and preparation, nanometer structure, activity and application thereof

A nanostructured, isoquinoline technology, used in the preparation of antithrombotic drugs, isoquinoline-3-formyl-Arg-Cys-OBzl, antithrombotic activity, its nano-resultant field, can solve cytotoxicity And other issues

Inactive Publication Date: 2016-01-06
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This form of cuttings can cause cytotoxicity

Method used

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  • Isoquinoline-3-formyl-RC-OBzl, and preparation, nanometer structure, activity and application thereof
  • Isoquinoline-3-formyl-RC-OBzl, and preparation, nanometer structure, activity and application thereof
  • Isoquinoline-3-formyl-RC-OBzl, and preparation, nanometer structure, activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1 prepares tetrahydroisoquinoline-3-carboxylic acid

[0021] Weigh 1g of L-phenylalanine, add 2.4mL of formaldehyde, and then add 8mL of 35% hydrochloric acid, the solution is first clarified and then a white substance precipitates out, and the reaction is carried out in an oil bath at 80°C for 8 hours. After the reaction, the solvent was removed and placed in an eggplant bottle. Diethyl ether was added and ultrasonically stirred for 1 hour, repeatedly ground and washed, and filtered to obtain 0.91 g (85%) of tetrahydroisoquinoline-3-carboxylic acid as a colorless solid. The melting point is 246-247°C. ESI-MS(m / e): 176[M-H] - .

Embodiment 2

[0022] Embodiment 2 prepares methyl tetrahydroisoquinoline-3-carboxylate

[0023] Add 6ml of methanol and 0.4ml of thionyl chloride to a 50ml eggplant-shaped bottle, stir, activate for 30min, and ice-bath. Add 239 mg of tetrahydroisoquinoline-3-carboxylic acid, and react under ice-cooling for 12 hours. The solvent was drained, methanol was added, and the solvent was drained 3 times; ether was added 3 times, and the solvent was drained to obtain 213 mg (82.5%) of methyl tetrahydroisoquinoline-3-carboxylate as a colorless powder. ESI-MS(m / e): 192[M+H] + .

Embodiment 3

[0024] Embodiment 3 prepares methyl isoquinoline-3-carboxylate

[0025] Dissolve 213 mg of methyl tetrahydroisoquinoline-3-carboxylate in anhydrous DMF, add potassium permanganate solution dissolved in distilled water, add slowly under ice bath, and react at room temperature for 24 hours. After the reaction, the DMF was blown dry, the black powder was dissolved with methanol and then filtered, and the filtrate was spin-dried. Separation and purification by column chromatography. 77 mg (37%) of methyl isoquinoline-3-carboxylate were obtained as a yellowish solid. Rf=0.25 (dichloromethane:methanol, 20:1); ESI-MS (m / e): 188[M+H] + ; 1 HNMR (DMSO-d 6 , 500MHz) δ / ppm=9.421(s, 1H), 8.666(s, 1H), 8.258(d, J=4Hz, 1H), 8.22(d, J=4Hz, 1H), 7.897(m, 2H), 3.944 (s, 3H).

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Abstract

The invention discloses isoquinoline-3-formyl-Arg(NG-NO2)-Cys(Bzl)-OBzl. The invention also discloses Arg(NG-NO2)-Cys(Bzl), a preparation method and antithrombotic activity thereof, and further discloses a nanometer structure of the Arg(NG-NO2)-Cys(Bzl) and application of the Arg(NG-NO2)-Cys(Bzl) in preparation of antithrombotic drugs.

Description

technical field [0001] The present invention relates to isoquinoline-3-formyl-Arg (N G -NO 2 )-Cys(Bzl)-OBzl, referred to as RC, relates to its preparation method, relates to its antithrombotic activity, and further relates to its nanometer results. Therefore the present invention relates to its application in the preparation of antithrombotic drugs. The invention belongs to the field of biomedicine. technical background [0002] Cancer is a general term for a group of diseases that can affect any part of the body. Other terms used are malignancy and neoplasm. According to the World Health Organization, cancer is one of the leading causes of death in the world, especially in developing countries. The number of cancer deaths worldwide is expected to continue to rise, exceeding 13.1 million by 2030. Therefore, the development of new anti-tumor drugs with high efficiency, low toxicity and small side effects has always been one of the important topics of new drug research....

Claims

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Application Information

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IPC IPC(8): C07K5/097C07K1/02A61K38/06A61P7/02B82Y30/00
Inventor 赵明彭师奇王玉记吴建辉王晓珍
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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