Synthesis process for anti-tumor new medicine 3-{(3-chlorphenyl)difluoromethyl-1-isopropyl-monohydro-pyrazolo(3,4-D)pyrimidine-4-amine compound

Abstract

The invention discloses a synthesis method for an anti-tumor new medicine 3-{(3-chlorphenyl)difluoromethyl-1-isopropyl-monohydro-pyrazolo(3,4-D)pyrimidine-4-amine compound. The synthesis method comprises the following steps of: acylating 3-chlorphenyl-2 oxalic acid serving as an initiative raw material; reacting the acylated material with dipropionitrile; performing methylation; performing ring closure with hydrazine hydrate to obtain 5-amino-1-(3-chlorophenyl)-pyrazole-4-carbonitrile, crystallizing and purifying, heating and performing ring closure with formamide to obtain a target mother ring; performing fluorination on carbonyl by using DAST; introducing difluorine into an active group so as to improve the bioactivity of the compound; performing process optimization on the basis of the compound; and performing the similar steps by using 2-(3-chlorphenyl)-2,2-difluoroacetic acid as a raw material to obtain the target product.

Description

technical field [0001] The present invention relates to the design and application of new antitumor drug 3-{(3-chlorophenyl)difluoromethyl-1-isopropyl-1hydro-pyrazolo(3,4-D)pyrimidine-4-amine compounds The synthesis belongs to the field of medicine and chemical technology. 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 mu...

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.

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