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New synthetic process of anticancer drug CF-102

A technology of CF-102 and anticancer drugs, which is applied in the new synthesis process field of anticancer drug CF-102, which can solve the problems of uneconomical reaction routes, high production costs, cumbersome operations, etc., and achieve low production costs and low equipment requirements , the effect of simple operation

Inactive Publication Date: 2019-07-12
江苏艾利瑞化学有限公司
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Problems solved by technology

[0004] The purpose of the present invention is to provide a new synthesis process of anticancer drug CF-102, to solve the above-mentioned background technology that the synthesis method of CF-102 currently on the market has many steps, complicated operation and high production cost, and, After condensation, it takes many steps to get the final product, and the reaction route is uneconomical

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  • New synthetic process of anticancer drug CF-102
  • New synthetic process of anticancer drug CF-102

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Embodiment Construction

[0016] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention.

[0017] see figure 1 , an embodiment provided by the present invention: a new synthesis process of anticancer drug CF-102, comprising the following steps:

[0018] Step 1: add compound a: 189g (1.0mol) 2,6-dichloropurine and 303g triethylamine (3mol) in 3000ml dry, clean there-necked flask, add 323.4g m-iodobenzylamine hydrochloride and 1200ml acetonitrile , Stir and heat up to produce substitution reaction, to reflux for 24h; Substitution reaction occurs, cool down to 0-5°C, crystallize for 2h, obtain light yellow solid weight, dry under reduced pressure at 60°C to constant weight, solid dry weight: 329.7g, mol Yield 85.5%, to obtain intermediate I;

[0019] Step 2...

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Abstract

The invention discloses a new synthetic process of an anticancer drug CF-102, and relates to the technical field of pharmaceutical production methods. The new synthetic process aims to solve problemsthat the synthetic method of CF-102 on the market has the characteristics of many steps, complicated operation and high production cost, and many steps are also needed to obtain a final product aftercondensation and the reaction route is not economical. The new synthetic process comprises the following steps: step 1: a compound a is used as a starting material, and a substitution reaction of thecompound a and m-iodobenzylamine hydrochloride is carried out to obtain an intermediate I; step 2: the intermediate I is condensed with a compound c to form a nucleoside bond to obtain an intermediateII; and step 3: amino-ester exchange and acetyl hydrolysis reaction of the intermediate II are synergistically carried out to obtain a final finished product.

Description

technical field [0001] The invention relates to a new synthesis process of an anticancer drug CF-102, and relates to the technical field of pharmaceutical production methods. Background technique [0002] CF102 is an oral small molecule drug, commonly known as Cl-IB-MECA (2-chloro-N6-(3-iodobenzyl)-adenosine-5'-N-methyluracil), A3 adenosine receptor A highly specific and selective agonist of A3AR. CF102 has potent anticancer effects, especially against hepatocellular carcinoma, and anti-inflammatory activity was shown in preclinical animal models of hepatitis. Its mechanism of action is mediated by deregulating NF-κB and Wnt signaling pathways, leading to tumor cell apoptosis. The protective effect of CF102 was mediated by down-regulating the NF-κB signaling pathway and preventing apoptosis. Its safety has been confirmed in preclinical studies, phase I clinical studies and human phase I / II clinical studies, showing a good safety profile. Phase I / II study in hepatocellula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18C07D473/34
CPCC07D473/18C07D473/34
Inventor 肖冬子王斌
Owner 江苏艾利瑞化学有限公司
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