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Synthesis method of three-function diagnosis and treatment integrated prodrug for prostate cancer and product thereof

A technology of prostate cancer and synthesis method, which is applied in the field of synthesis of three-function diagnosis and treatment integrated precursor drugs, can solve the problems of limiting the production and sales of PSMAI&T drugs, lack of availability, and low yield

Pending Publication Date: 2021-09-07
SUZHOU SITRI ISOTOPE TECH RES INSITITUTE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

in 68 Ga is mainly used for imaging diagnosis, but due to its high production cost and low yield (by 68 Ge / 68 Ga generator), most hospitals currently do not have independent production 68 Ga contrast agent capability while 68 The half-life of Ga is short, only 68 minutes, and it can only be produced and used now. If it is professionally produced and distributed by a third-party organization, taking into account the road factor (the general road time is 2 hours), only 1 / 4 of the original output will be left in the hands of customers. Therefore, it is basically impossible to achieve commercial production, which seriously limits the production and sales of PSMA I&T drugs.

Method used

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  • Synthesis method of three-function diagnosis and treatment integrated prodrug for prostate cancer and product thereof
  • Synthesis method of three-function diagnosis and treatment integrated prodrug for prostate cancer and product thereof
  • Synthesis method of three-function diagnosis and treatment integrated prodrug for prostate cancer and product thereof

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preparation example Construction

[0040] Such as Figure 1-5 Shown, a kind of synthetic method of the prodrug precursor of three-function diagnosis and treatment integration for prostate cancer, comprises the following steps:

[0041] (1) Using 1.00eq of compound 1 as a raw material, drop compound 1 into the active ester solution, suction filter, wash and dry after the stirring reaction is complete, to obtain compound 2; the solvent of the active ester solution is preferably dimethylformamide; The molar ratio of compound 1 to active ester solution is 1:1.10-2.00, the reaction temperature is room temperature, and the amino group reaction is judged to be complete through the color reaction;

[0042] (2) Put compound 2, amino acid 1, and aprotic polar solvent obtained in step (1) into a reaction flask for mixing, then add an organic base dropwise, stir and react, and obtain compound 3 by suction filtration, washing and drying;

[0043] (3) Add piperidine solution to compound 3, and obtain compound 4 after reacti...

Embodiment 1

[0058] Such as Figure 1-2 Shown, a kind of synthetic method of the prodrug precursor of three-function diagnosis and treatment integration for prostate cancer, comprises the following steps:

[0059] (1) Using compound 1 (1.00eq) as a raw material, drop compound 1 (5.08g, 2.69mmol) into 10mL active ester in dimethylformamide solution (containing active ester 1.77g, 4.02mmol), at room temperature The mixture was stirred and reacted for 3 hours, and the color reaction showed that the amino group had basically reacted completely, then suction filtered, washed and dried with dimethylformamide solution, and compound 2 was obtained;

[0060] (2) the above-mentioned compound 2, amino acid 1 (3.45g, 8.14mmol) and dimethylformamide (10mL) were added to the reaction flask, and N,N-diisopropylethylamine (1.02g, 7.89mmol) was added dropwise at room temperature, and the reaction was stirred at room temperature for 3h, Suction filtration, washing and drying with dimethylformamide to obt...

Embodiment 2

[0070] Such as Figure 1-2 Shown, a kind of synthetic method of the prodrug precursor of three-function diagnosis and treatment integration for prostate cancer, comprises the following steps:

[0071] (1) Using compound 1 (1.00eq) as raw material, drop compound 1 (4.74g, 2.51mmol) into 10mL of active ester in dimethylformamide solution (containing active ester 1.22g, 2.77mmol), at room temperature The mixture was stirred and reacted for 4 hours, and the color reaction showed that the amino group had basically reacted, then suction filtered, washed and dried with dimethylformamide solution, and compound 2 was obtained;

[0072] (2) the above-mentioned compound 2, amino acid 1 (2.13g, 5.03mmol) and dimethylformamide (10mL) were added to the reaction flask, and N,N-diisopropylethylamine (0.65g, 5.04mmol) was added dropwise at room temperature, and the reaction was stirred at room temperature for 2~ 8h, suction filtration, washing and drying with dimethylformamide to obtain com...

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Abstract

The invention discloses a synthesis method of a three-function diagnosis and treatment integrated prodrug for prostate cancer and a product thereof. A compound 1 is used as a raw material, and the compound 1 and three different amino acids are used to gradually synthesize the three-function diagnosis and treatment integrated prodrug, so that the prodrug can obtain the ability to mark three radionuclides of 18F, 68Ga and 177Lu. The invention realizes that the marking rate of 18F reaches 40%, and the marking rate of 68Ga and 177Lu reaches 90% or more, and can be combined with other targeting molecules other than PSMA to design more bifunctional or trifunctional diagnostic drugs, the structure will greatly open the PSMA structure drug market, provide more, more flexible, more functional radionuclide marker options for such type of drugs, and have a great promotion effect on the diagnosis and treatment of prostate cancer, which is suitable for industrial popularization and use.

Description

technical field [0001] The invention belongs to the technical fields of chemical synthesis, labeling, imaging, drug therapy and prostate cancer treatment, and specifically relates to a synthesis method and a product thereof for a prodrug integrated with three functions for diagnosis and treatment of prostate cancer. Background technique [0002] Prostate cancer (English full name Prostate Cancer, English abbreviation PCa) refers to epithelial malignant tumors that occur in the prostate gland. It is one of the most common malignant tumors in men. It is estimated that there will be more than 11 million prostate cancer patients worldwide in 2022. For details, see Siegel RL, Miller KD, Jemal A. Cancer statistics, 2020. CA Cancer J Clin 2020;70:7-30. In recent years, the incidence of prostate cancer in my country has also shown an obvious upward trend. As of 2020, the number of new patients with prostate cancer in my country has reached 153,000, and it is expected to reach 237,00...

Claims

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Application Information

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IPC IPC(8): C07K5/02C07K1/02
CPCC07K5/0207
Inventor 桂媛陈伟徐志红沈佳宇李维宽
Owner SUZHOU SITRI ISOTOPE TECH RES INSITITUTE CO LTD
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