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Camptothecin derivative used as anti-tumor agent and preparation method thereof

A technology of drugs and compounds, applied in the field of new derivatives of camptothecin, which can solve the problems of anti-tumor activity and unsatisfactory low toxicity

Inactive Publication Date: 2007-06-06
HEFEI KEDA BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antitumor activity and low toxicity of these new derivatives of camptothecin are still not ideal

Method used

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  • Camptothecin derivative used as anti-tumor agent and preparation method thereof
  • Camptothecin derivative used as anti-tumor agent and preparation method thereof
  • Camptothecin derivative used as anti-tumor agent and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0059] 105mg (0.3mmol) of camptothecin was first dissolved in 15mL of methanol, then 1.2 equivalents of N-(3-propylamino)morpholine was added, and reacted at 75°C for 14 hours. After the system became clear, the reaction mixture was Pour it into 80 mL of diethyl ether, a yellow precipitate precipitated out, filtered off the precipitate, and washed the crude product with 2×2 mL of cold diethyl ether. It can be seen from TLC that the crude product contains unreacted camptothecin starting material. Dissolve the crude product in a small amount of CHCl 3 , further purified with alumina column chromatography (eluent: ethyl acetate:petroleum ether 1:4->1:1) to obtain 106g of pure compound of formula (I), yield 88%, HPLC showed its purity 99.1%.

[0060] IR(KBr)ν: 1620cm -1 (-CO-NH-)

[0061] 1 H NMR: (CDCl 3 , 300MHz) δpm: 1.07 (t, J=7.2Hz, 3H, 18-CH 3 ); 1.76(q, 2H, 19-CH 2 ); 2.25 (m, 1H, 23-CH 2 ), .2.43(m, 1H, 23-CH 2 ); 2.44(m, 4H, 2×25-CH 2 ); 3.41 (m, 2H, 22-CH 2 )...

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Abstract

The invention discloses a camptothecine derivative used as an antineoplastic agent and its preparing process, wherein formula (1) represents the camptothecine derivative.

Description

Field of invention: [0001] The invention relates to a novel camptothecin derivative used as an antitumor agent, its preparation method and use as an antitumor agent. Background of the invention: [0002] Camptothecin is an alkaloid extracted from the plants of the family Cotoneasteraceae in my country, which has strong antitumor activity. Its structure is as follows: [0003] [0004] Formula (II) [0005] However, camptothecin itself is limited in its application due to its high toxicity and side effects, and many new compounds with high activity and low toxicity have been approved for clinical treatment among its derivatives. For example, Irinotecan (Irrinotican) and Topotecan (Topotican) etc. Some new compounds with activity equal to or better than camptothecin and less toxic than camptothecin have also been found in the ring-opened derivatives of the E lactone ring of camptothecin. Some of them are soluble in water, so they are suitable for mak...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/14A61K31/5377A61K9/08A61K9/00A61P35/00
Inventor 尤田耙李明宗王宗贵耿燕
Owner HEFEI KEDA BIO TECH CO LTD