Novel synthesis process of capecitabine

A technology of capecitabine and synthesis process, which is applied in the direction of organic compound/hydride/coordination complex catalyst, preparation of sugar derivatives, sugar derivatives, etc. It can solve the problems of heavy metal pollution and high cost, and achieve total revenue High efficiency, simple post-treatment, and the effect of avoiding heavy metal pollution

Active Publication Date: 2013-05-15
湖南欧亚药业有限公司
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Problems solved by technology

[0018] The method for synthesizing capecitabine, the first two methods do not have too much description for the three-dimensional configuration of the product, and the latter two methods use different methods to obtain the required capecitabine in the β configuration, but also All there are some deficiencies, method three adopts tin tetrachloride as catalyst, has heavy metal pollution, and the ammonium sulfate, HMDS method cost that method four adopts is higher

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  • Novel synthesis process of capecitabine
  • Novel synthesis process of capecitabine
  • Novel synthesis process of capecitabine

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Embodiment Construction

[0033] In order to make the technical means, creative features, work flow, and use methods of the present invention achieve the purpose and effect easily understood, the present invention will be further described below in conjunction with specific embodiments.

[0034]

[0035]

[0036]

[0037] Synthesis of Compound II:

[0038] 134 grams of compound Ⅰ (1.00mol) was added to 800 milliliters of N,N-dimethylformamide, under stirring, 8.6 grams of p-toluenesulfonic acid (0.05mol) was added, and 124.8 grams of 2,2-dimethoxy Propane (1.20mol), stirred at room temperature overnight, after the reaction, concentrated under reduced pressure to distill unreacted 2,2-dimethoxypropane and N,N-dimethoxypropane, the residue was added to 500ml of water, Use 10% sodium carbonate aqueous solution to adjust PH=7-8, add 1200 ml of ethyl acetate for extraction, the ethyl acetate layer is washed with saturated brine, and dried over anhydrous sodium sulfate; filter, and the filtrate is c...

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Abstract

The invention discloses a novel synthesis process of capecitabine and discloses a preparation method of 2',3'-O-isopropylidene-5'-deoxy-5-fluoro-N4-(carbopentyloxy)cytimidine (compound V) serving as an intermediate. Meanwhile, the invention discloses a preparation method for obtaining capecitabine by removing a protective group from the compound serving as a raw material under the catalytic action of iodine. The method has the advantages of readily available raw materials, environmental friendliness, high yield and no heavy metal pollution, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a novel synthesis process of capecitabine. Background technique [0002] Capecitabine (Capecitabine), trade name Xeloda, chemical name 5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl] cytosine nucleoside, is a new type of drug developed by Roche, Switzerland Oral fluoropyrimidine anti-tumor is a new type of capecitabine synthetic technology tumor drug, which has selective anti-tumor activity. Capecitabine itself has no cytotoxicity, and through a unique three-step enzymatic reaction in vivo, it is converted into 5-fluorouracil (5-Fu) in tumor cells to play a highly selective anti-tumor effect, with obvious cell targeting And simulate the pharmacokinetic properties of continuous 5-Fu intravenous infusion, it has strong activity against a variety of solid tumors, and is an oral cytotoxic preparation with selective effects on tumor cells. Approved by the US FDA in September 1998, it is clinically used to treat advanced primary or metas...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/06C07H1/00B01J31/02
CPCY02P20/55
Inventor 林开朝
Owner 湖南欧亚药业有限公司
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