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Novel synthesis process of anti-cancer Sunpla

A new process, anti-cancer drug technology, applied in the field of biopharmaceuticals, can solve the problems of long processing process, introduction of silver impurities, affecting product quality, etc., and achieve the effect of short synthesis route, improved product quality, and high yield

Inactive Publication Date: 2009-06-10
KUNMING GUIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] There are following shortcomings and deficiencies in the synthesis method of Suplatin used in existing patents and documents: First, because silver compounds are used in the synthesis, silver impurities will be introduced in the final product Suplatin, which will affect the quality of the product
Dispersion and loss of Pt due to long process, expressed in K 2 PtCl 4 Calculated as the starting material, the loss of metal platinum reaches 5%, which greatly increases the production cost of Shubo

Method used

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  • Novel synthesis process of anti-cancer Sunpla
  • Novel synthesis process of anti-cancer Sunpla
  • Novel synthesis process of anti-cancer Sunpla

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] (1), the preparation of two (malonate) platinum (II) potassium

[0018] Take 10g (24mmol) K 2 PtCl 4 , dissolved in 100ml of water, added 35g (192mmol) CH 2 (COOK) 2 and 4.9g (48mmol) CH 2 (COOH) 2 , reacted at 75°C for 8 hours, cooled, precipitated yellow crystals, collected by filtration, washed with water and ethanol, and dried in vacuum at 65°C for 4 hours to obtain 9.63g K 2 {Pt[CH 2 (COO) 2 ] 2} 2H 2 O, 85% yield.

[0019] The characteristic structural parameters are: . Elemental analysis C 14.11%; H 1.57%; Pt 38.2%, consistent with the theoretical value C 14.04%; H 1.560%; Pt 38.0%. .FAB + -MS m / e=400 (Pt[CH 2 (COO) 2 ] 2+ , 45%). .IR(cm -1 , KBr tablet) 3572-3495 (s, vO-H, H 2 O) 2861 (w, vCH2), 1635 [vs vas (COO)], 1370 [svs (COO)]. These parameters conform to K 2 {Pt[CH 2 (COO) 2 ] 2} 2H 2 The chemical structure of O.

[0020] (2), the synthesis of Platinum

[0021] Take 4g (7.8mmol) K 2 {Pt[CH 2 (COO) 2 ] 2} 2H 2 O, dissolved in ...

Embodiment 2

[0028] (1), the preparation of two (malonate) platinum (II) sodium

[0029] Take 9.2g (24mmol) Na 2 PtCl 4 , dissolved in 100ml of water, added 28.4g (192mmol) CH 2 (COONa) 2 and 4.9g (48mmol) CH 2 (COOH) 2 , reacted at 75°C for 8 hours, cooled, precipitated pale yellow crystals, collected by filtration, washed with water and ethanol, and dried in vacuum at 65°C for 4 hours to obtain 7.5g Na 2 {Pt[CH 2 (COO) 2 ] 2} H 2 O, yield 75%, Pt42.8%.

[0030] (2), the synthesis of Platinum

[0031] Take 3.55g (7.8mmol) Na 2 {Pt[CH 2 (COO) 2 ] 2} 2H 2 O, dissolved in 20ml of water, slowly add 1.6g (9.2mmol) of (4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxo After cyclopentane, it was heated to reflux for 12 hours, cooled, off-white crystals were precipitated, collected by filtration, washed with water and ethanol, and then vacuum-dried at 65° C. for 4 hours to obtain 2.34 g of splatin, with a yield of 65%.

[0032] (3), the purification of Shuplatin

[0033] Take 2g...

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Abstract

The related new synthesis technique for Sunpla or Eptaplatin comprises: preparing the complex of M2{Pt[CH2(COO)2]2} with M2PtCl4 and CH2(COOM)2; then reacting with the carrier group of amine(4R, 5R)-4, 5-bi(aminomethyl)-2-isopropyl-1, 3-cyclopentane dioxide. This invention has high yield with short synthesis path and no harmful Ag and Hg to provide high-pure bulk drug.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to a synthesis and preparation process of platinum-based anticancer drug Sunpla. Background technique [0002] Sunpla, also known as Eptaplatin or Eptaplatin, its chemical name is cis-[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3 -Dioxolane] (malonate) platinum (II), the structural formula is as follows, it is a new type of platinum anticancer drug developed by Sunkyong Industries Life Science Research Center in South Korea, and it was approved for marketing in South Korea in 1999. The main indications are gastric cancer, small cell lung cancer, head and neck cancer, colorectal cancer, uterine cancer, etc. Liu Weiping. Platinum group metal complexes for cancer treatment. Advances in Pharmacy, 2001, 25(1), 27-30; edited by Peng Sixun. Advances in Pharmacy, 2003, 2, 161-187]. Due to the remarkable clinical curative effect of Shubo, Sunkyong Industries is currently applying for mark...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61P35/00
Inventor 刘伟平谌喜株高文桂刘洋余尧何键普绍平
Owner KUNMING GUIYAN PHARMA
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