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A new crystal form of 7-ethyl-10-hydroxycamptothecin and its preparation method

A technology of hydroxycamptothecin and crystal form, applied in the field of medicinal chemistry, can solve the problem of low solubility of polymorphs, and achieve the effects of simple and easy operation and high solubility of the preparation method

Active Publication Date: 2016-03-30
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the polymorphic form of 7-ethyl-10-hydroxycamptothecin is not very soluble

Method used

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  • A new crystal form of 7-ethyl-10-hydroxycamptothecin and its preparation method
  • A new crystal form of 7-ethyl-10-hydroxycamptothecin and its preparation method
  • A new crystal form of 7-ethyl-10-hydroxycamptothecin and its preparation method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1, the preparation of 7-ethyl-10-hydroxycamptothecin crystal form

[0031] Weigh 50mg of 7-ethyl-10-hydroxycamptothecin into a reaction flask, add 1.5ml of dimethyl sulfoxide, stir to dissolve, evaporate the solvent at 20-30°C to crystallize, and separate the solid by filtration. Vacuum-dry to constant weight to obtain the crystal form of 7-ethyl-10-hydroxycamptothecin.

Embodiment 2

[0032] Embodiment 2, the preparation of 7-ethyl-10-hydroxycamptothecin crystal form

[0033] Weigh 30mg of 7-ethyl-10-hydroxycamptothecin into a reaction flask, add 1.5ml of dimethyl sulfoxide, stir to dissolve, the volatile solvent crystallizes at 20-30°C, filter and separate the solid, and the solid at 50°C Vacuum-dry to constant weight to obtain the crystal form of 7-ethyl-10-hydroxycamptothecin.

Embodiment 3

[0034] Embodiment 3, the preparation of 7-ethyl-10-hydroxycamptothecin crystal form

[0035] Weigh 30mg of 7-ethyl-10-hydroxycamptothecin into a reaction flask, add 3ml of N,N-dimethylformamide, stir to dissolve, add dropwise to 2ml of ethyl acetate solution, crystallize the volatile solvent at room temperature, filter The solid was separated, and the solid was vacuum-dried at 50° C. to constant weight to obtain the crystal form of 7-ethyl-10-hydroxycamptothecin.

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Abstract

The invention relates to a novel 7-ethyl-10-hydroxycamptothecine crystal and a preparation method thereof. According to the novel 7-ethyl-10-hydroxycamptothecine crystal, X-ray powder which is radiated by using Cu-Ka and expressed through a 2 theta angle has characteristic peaks at diffraction angles of 7.1 degrees, 10.26 degrees, 11.36 degrees, 13.22 degrees, 14.14 degrees, 16.12 degrees, 17.86 degrees, 18.74 degrees, 19.5 degrees, 20.18 degrees, 21.98 degrees, 22.74 degrees, 23.64 degrees, 24.6 degrees, 25.28 degrees, 26.52 degrees and 29.84 degrees, and the error range of 2 theta is + / -0.2 degree. The novel 7-ethyl-10-hydroxycamptothecine crystal disclosed by the invention is high in solubility. The preparation method disclosed by the invention is simple, easy to operate and suitable for technical production.

Description

technical field [0001] The invention relates to a new crystal form of 7-ethyl-10 hydroxycamptothecin and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] Irinotecan (mnotecan, CPT-11) is a semi-synthetic water-soluble derivative of camptothecin. Its antitumor activity is higher than that of camptothecin, and its side effects are lower than that of camptothecin. The anti-tumor mechanism of irinotecan is mainly to inhibit the activity of topoisomerase-I, which affects DNA replication and leads to cell death. CPT-11 is an important drug for the treatment of small-cell lung cancer (SCLC). In 2010, the National Comprehensive Cancer Network (NCCN) in the United States recommended CPT-11 as the first-line treatment drug for advanced SCLC, and it can also be used for second-line treatment. . Irinotecan is an ester prodrug, which is mainly metabolized by carboxylesterase into 7-ethyl-10-hydroxycamptothecin (SN-38) ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/22A61K31/4745A61P35/00
CPCC07D491/22
Inventor 王蕾房兰陶绪堂仵泽鑫
Owner SHANDONG UNIV
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