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A kind of synthetic technology of antineoplastic drug chlorambucil

A chlorambucil and a synthesis process technology, applied in the preparation of organic compounds, organic chemistry, chemical instruments and methods, etc., can solve the problems of high toxicity, high cost, low yield and the like

Active Publication Date: 2016-10-05
PINGHU UCON PHARMA R&D
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  • Claims
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Problems solved by technology

[0005] There have been some reports on the synthesis process of chlorambucil at present, but the ubiquitous cost is high, the yield is low, and the shortcomings of high toxicity

Method used

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  • A kind of synthetic technology of antineoplastic drug chlorambucil
  • A kind of synthetic technology of antineoplastic drug chlorambucil

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Embodiment Construction

[0027] The present invention will be further described below in conjunction with specific examples.

[0028] Step (1) amino protection reaction:

[0029] Mix 93.2g of aniline and 900g of water into a 2000ml three-necked flask, stir mechanically, control the temperature below 45°C, add 103.2g of acetic anhydride, stir for 20min, filter, wash the filter cake with water, and dry it at 60°C to obtain white luster Crystalline powder 104g, the yield is 81%.

[0030] Step (2) acylation reaction:

[0031] Add 400g of aluminum chloride and 800ml of dichloromethane into a 3L three-necked flask, cool in an ice bath, mix 160g of acetanilide and 120g of succinic anhydride and add in portions, remove the ice bath after 15 minutes, react at room temperature for half an hour, and let it stand After 2-3 days, add ice water (about 1.5Kg) to generate a large amount of hydrogen chloride gas, stir, filter, wash with water, dissolve the filter cake with 4N aqueous sodium hydroxide solution, extra...

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Abstract

The invention relates to a synthesis process of an antineoplastic drug chlorambucil. The synthesis process comprises the following steps: (1) amino protection reaction; (2) acylation reaction; (3) reduction reaction; (4) carboxyl protection reaction; (5) substitution reaction; (6) chlorination reaction; and (7) deprotection reaction. According to the synthesis process, the amino group is protected by use of acetic anhydride, and then acylation, reduction, carboxyl protection, substitution, chlorination and aqueous hydrochloric acid solution hydrolysis are performed to obtain the chlorambucil. The synthesis process of the antineoplastic drug chlorambucil has the characteristics of low cost, mild reaction conditions, low toxicity, convenience in process operation, and suitability for industrial production.

Description

technical field [0001] The invention relates to a synthesis process of an antineoplastic drug chlorambucil (Chlorambucil), which belongs to the field of drug synthesis. Background technique [0002] Chlorambucil, its chemical name is 4-[4-(dichloroethylamino)phenyl]butyric acid (4-(p-bis(2-chloroethyl)aminophenyl)butyric acid), its structural formula is: [0003] [0004] Chlorambucil is a derivative of nitrogen mustard, an antineoplastic drug-cytotoxic drug-a drug that acts on the chemical structure of DNA, a bifunctional alkylating agent, a non-specific drug for the cell cycle, and forms unstable ethylene It can selectively act on lymphoid tissue, interfere with the function of DNA and RNA, and has the strongest effect on cells in the M phase and G1 phase of the cell cycle. Chlorambucil has a good effect on Cheeter's syndrome (genital ulcer, aphthous ulcer and uveitis syndrome), lupus erythematosus and Wegener's granulomatosis. It has a good effect in the treatment of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C229/40C07C227/18
Inventor 忻华钟全发史黎辉
Owner PINGHU UCON PHARMA R&D
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