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Method for purifying vindesine

A purification method, the technology of vindesine, which is applied in the direction of organic chemistry, can solve the problems of complicated process and low purification efficiency of vindesine, and achieve the effect of strong operability

Inactive Publication Date: 2015-09-09
GUANGZHOU HANFANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the problems of low purification efficiency and complex process of vindesine, the purpose of the present invention is to provide a purification method of vindesine with high purity, strong operability and suitable for industrial production

Method used

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  • Method for purifying vindesine
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  • Method for purifying vindesine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1) Weigh 5.98kg of 300-mesh silica gel, add chloroform and stir to remove the air bubbles in the silica gel, and then evenly load the silica gel into the preparative chromatography. The column size is Φ20cm×52cm. After the stationary phase silica gel is compacted, rinse with the eluent 2h, to obtain the preparative chromatographic column packed;

[0027] 2) Dissolve 195g of Vindesin crude product (purity is 76.73%) in chloroform, feed, feed amount is 300ml;

[0028] 3) Use a constant pressure and constant flow pump to enter the eluent, first use chloroform: methanol = 90: 1 solvent to elute 2 bed layers, then use chloroform: methanol = 40: 1 solvent to elute 3 bed layers and collect the elution Solution a, then use chloroform:methanol=30:1 solvent to elute the 4 bed layers and collect eluent b, and finally replace it with chloroform:methanol=15:1 eluent to elute the residue in the prepared chromatographic column;

[0029] 4) The eluent b was recovered under reduced pre...

Embodiment 2

[0032] 1) Weigh 6.10kg of 400-mesh silica gel, add chloroform and stir to remove the air bubbles in the silica gel, and then evenly load the silica gel into the preparative chromatography. The column size is Φ20cm×52cm. After the stationary phase silica gel is compacted, rinse with the eluent 2h, to obtain the preparative chromatographic column packed;

[0033] 2) Dissolve 205g of Vindesin crude product (purity is 72.19%) in chloroform, feed, feed amount is 320ml;

[0034] 3) Use a constant pressure and constant flow pump to enter the eluent, first use chloroform:methanol=95:1 solvent to elute 2 bed layers, then use chloroform:methanol=45:1 solvent to elute 3 bed layers and collect the elution solution a, then use chloroform:methanol=35:1 solvent to elute 4 bed layers and collect eluent b, and finally use chloroform:methanol=15:1 eluent to elute the residue in the prepared chromatographic column;

[0035] 4) The eluent b was recovered under reduced pressure to obtain 94.5 g o...

Embodiment 3

[0037] 1) Weigh 6.00kg of 200-mesh silica gel, add chloroform and stir to remove the air bubbles in the silica gel, and then evenly load the silica gel into the preparative chromatography. The column size is Φ20cm×52cm. After the stationary phase silica gel is compacted, rinse with the eluent 2h, to obtain the preparative chromatographic column packed;

[0038] 2) Dissolve 165g of Vindesin crude product (purity: 58.97%) in chloroform, feed, feed amount is 280ml;

[0039] 3) Use a constant pressure and constant flow pump to enter the eluent, first use chloroform: methanol = 90: 1 solvent to elute the 3 beds, then use chloroform: methanol = 40: 1 solvent to elute the 3 beds and collect the elution solution a, and then use chloroform:methanol=30:1 solvent to elute the 4 bed layers and collect the eluent b, and finally replace it with chloroform:methanol=10:1 eluent to elute the residue in the prepared chromatographic column;

[0040] 4) The eluent b was recovered under reduced p...

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Abstract

The invention discloses a method for purifying vindesine. The method for purifying the vindesine comprises the following steps of: (1) preparing a chromatographic column from a chromatographic column filler, wherein silica gel, which is swollen by an organic solvent A, serves as the chromatographic column filler; (2) adding a vindesine crude product organic solvent A solution into the chromatographic column; (3) eluting the chromatographic column by a gradient elution method and by sequentially using eluent consisting of organic solvent A / organic solvent B mixed liquid with gradually reduced volume ratio, collecting main component effluent and finally washing out residues; and (4) concentrating under reduced pressure and recycling eluent to obtain high-purity vindesine. The product obtained by the method has high purity. By the method, the purity of the vindesine can reach to more than 90% and the yield of the vindesine can be 40-80%. A stationary phase is stable and can be reused.

Description

technical field [0001] The invention relates to a purification technology of vindesine, in particular to a purification method of vindesine. Background technique [0002] Vinblastine compounds are alkaloids extracted from Catharanthus roseus (Catharanthus roseus), which have anti-tumor activity and are mainly used to treat malignant tumors such as non-small cell lung cancer, small cell cancer, breast cancer, and malignant lymphoma . Vinblastine, vincristine, vindesine and vinorelbine have been officially used clinically. Among them, vindesine is a typical 4-deacetyl-C-3 amide derivative obtained by modifying the 3 and 4 positions of the vinblastine G ring, which can form a covalent bond with the circulating glycoprotein in the cell-transferrin, thereby Breaking its combination with iron leads to apoptosis of tumor cells, the structural formula is as follows. [0003] [0004] Domestic research mainly focuses on the modification of dosage forms and drug combinations of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/04
CPCC07D519/04
Inventor 宋晓燕颜景胡袁诚李金华傅玉萍林秀仙潘振华李咏华
Owner GUANGZHOU HANFANG PHARMA
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