Water-soluble stable lobaplatin derivative

A derivative, the technology of lobaplatin, applied in the field of water-soluble and stable derivatives of lobaplatin, can solve the problems of poor chemical stability, weak coordination ability, inconvenient clinical use, etc., and achieve good water solubility and high anticancer effect , the effect of good clinical application prospects

Inactive Publication Date: 2014-05-07
KUNMING INST OF PRECIOUS METALS +1
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Problems solved by technology

However, L-lactic acid is an a-hydroxy acid, and the oxygen on the hydroxyl group has a weak coordination ability with platinum (), so it is easy to Dissociated from platinum (), therefore, the chemical stability of lobaplatin is poor, and its aqueous solution is only stable for 4 hours. It is required to be used within 4 hours after clinically formulated as an injection, and the stability time in normal saline is 1.5-4 hours [Instructions for Lobaplatin for Injection; China New Drug Impurities, 2012, 21(19), 2321- 2325], it is inconvenient to use clinically, and improper use will also affect the curative effect

Method used

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  • Water-soluble stable lobaplatin derivative
  • Water-soluble stable lobaplatin derivative
  • Water-soluble stable lobaplatin derivative

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Embodiment Construction

[0019] (1) Diiodine intermediate ( 1 ) preparation of

[0020] The carrier amine of Xinluoplatin trans-1,2-bis(aminomethyl)cyclobutane was synthesized according to the method reported in the literature [8]. Then, take 5 g (12 mmol) K 2 PtCl 4 , Dissolve in 80 ml of water, take 12 g (6×12 mmol) KI, dissolve in 20 ml of water, mix the two solutions at 35-40°C in the dark, after 2 hours, add trans- 20 ml of 1,2-bis(aminomethyl)cyclobutane solution (including 1.37 g, 12 mmol), a brownish-yellow precipitate precipitated, continued to stir for 4 hours, collected by filtration, washed with water and ethanol respectively, and vacuumed at 45°C Dry to obtain 6.28 g cis-[trans-1,2-bis(aminomethyl)cyclobutane diiodoplatinum ( )]( 1 ), the yield was 93%.

[0021] (2) Preparation of silver 3-hydroxy-1,1-cyclobutanedicarboxylate (2)

[0022] The leaving group 3-hydroxy-1,1-cyclobutanedicarboxylic acid was prepared according to the method of literature [9]. Take 3 g (19 mmol) of...

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Abstract

The invention discloses a water-soluble stable lobaplatin derivative, namely, shionlobaplatin. The chemical name of the shionlobaplatin is cis-[trans-1,2-bis(aminomethyl) cyclobutane 3-hydroxy-1,1-cyclobutane dicarboxylate platinum as shown in the specification. The preparation of the water-soluble stable derivative shionlobaplatin comprises the steps of by taking K2[PtCl4] as a starting raw material in water, adding KI to the K2[PtCl4] so that K2[PtCl4) is transformed into K2PtI4, reacting the K2PtI4 with trans-1,2-bis(aminomethyl) cyclobutane to prepare a corresponding diiodine intermediate, and then carrying out an equimolar quantitative reaction between the diiodine intermediate and 3-hydroxy-1,1-cyclobutane dicarboxylic acid to obtain the target compound. The compound shionlobaplatin has the characteristics of good water solubility, high stability and high anti-cancer effect, and can be prepared into a freeze-dried powder or an aqueous solution for clinical treatment of cancers.

Description

technical field [0001] The invention relates to a stable water-soluble lobaplatin derivative-cis-[trans-1,2-bis(aminomethyl)cyclobutane 3-hydroxyl-1,1-cyclobutane dicarboxylic acid platinum ( )] (English name: cis-[trans-1.2-bis (methylamine)cyclobutane3-hydroxy-1,1-cyclobutanedicarboxylatoplatinum ( )]) and as an anticancer drug, belonging to the field of chemical pharmacy. Background technique [0002] Platinum drugs are a very important class of anticancer drugs and are the first choice for the treatment of common malignant tumors [Edited by Han Rui, Sun Yan. Chemoprevention and Drug Therapy of Cancer in the New Century. People's Military Medical Publishing House , 2005, Beijing], widely used in clinical treatment of cancer, according to the latest statistics, currently 50% of clinical combined chemotherapy regimens are based on platinum drugs or participate in compatibility [Dhar S & Lippard S J. Mitaplatin, a potent fusion of cisplatin and the orphan drug dichloroa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/282A61P35/00A61P35/02
Inventor 刘伟平楼丽广谌喜珠谢成英姜婧叶青松全海天常桥稳
Owner KUNMING INST OF PRECIOUS METALS
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