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New synthesis process of new antineoplastic drug INK128

A technology of a process and a synthetic route, applied in the field of synthesis of new anti-tumor drugs, can solve the problems of non-response or drug resistance of cancer patients, threatening human life and health, and treatment failure.

Inactive Publication Date: 2012-09-05
CGENETECH (SUZHOU CHINA) CO LTD
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  • Abstract
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AI Technical Summary

Problems solved by technology

[0002] Nearly 50 years of research and development of anti-tumor drugs have made considerable progress in cancer chemotherapy, especially prolonging the survival time of patients with hematological malignancies, but the treatment of solid tumors, which seriously threaten human life and health and account for more than 90% of malignant tumors, has not yet been developed. Satisfactory curative effect has been achieved, but half of the cancer patients still do not respond to or resist the treatment and eventually lead to treatment failure
Therefore, discovering and developing new antitumor drugs is still a very arduous and long-term mission and challenge that pharmacists must face.

Method used

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  • New synthesis process of new antineoplastic drug INK128

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Embodiment Construction

[0012] Preparation of compound (b):

[0013] Dissolve 152 g (1 mole) of starting material (a) in 1.5 liters of dichloromethane, add 5 milliliters of DMF and then dropwise add 254 g (2 moles) of oxalyl chloride. Under ice-water cooling, the dropwise temperature rises to room temperature and stirs for 3 hours. , spin-dried to obtain 171 g of acid chloride (yield 100%), which was directly used in the next step without purification.

[0014] Preparation of compound (c):

[0015] Dissolve 66 grams (1 mole) of propanedinitrile in 660 milliliters of DMF, cool to 0 degrees, add 44 grams (1.1 moles) of sodium hydrogen (60% purity) in batches, react at room temperature for 1 hour after the addition, and cool in an ice-salt bath Add the acid chloride obtained in the step dropwise, control the temperature below 5°C, and react overnight at room temperature after completion, the reaction is complete as detected by TLC, the reaction solution is poured into 1 liter of ice water, extracted th...

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Abstract

The invention discloses a new synthesis process of a new antineoplastic drug INK128, which comprises the following steps: acylating the initial raw material p-methoxybenzoic acid, reacting with malononitrile, methylating to cyclize with hydrazine hydrate to obtain 3-amino-5-(4-methoxyphenyl)-pyrazolyl-4-nitrile, purifying by crystallization, heating to cyclize with formamide to obtain the target mother cycle, alkylating, nitrifying, deprotecting, reducing, and finally, cyclizing with cyanogen bromide.

Description

technical field [0001] The invention relates to a synthesis process of a new antitumor drug, belonging to the technical fields of medicine and chemical industry. Background technique [0002] Nearly 50 years of research and development of anti-tumor drugs have made considerable progress in cancer chemotherapy, especially prolonging the survival time of patients with hematological malignancies, but the treatment of solid tumors, which seriously threaten human life and health and account for more than 90% of malignant tumors, has not yet been developed. Even if a satisfactory curative effect is achieved, half of the cancer patients still have no response or drug resistance to treatment, which eventually leads to treatment failure. Therefore, discovering and developing new antitumor drugs is still a very arduous and long-term mission and challenge that pharmacists must face. With the rapid development of molecular oncology and molecular pharmacology, the nature of tumors can b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
Inventor 张福治余强丁炬平张仁延
Owner CGENETECH (SUZHOU CHINA) CO LTD
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