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Preparation method of anagrelide derivative

A technology for derivatives and substances, applied in the field of drug synthesis, can solve the problems of unreported synthetic methods of anagrelide derivatives, and achieve the effects of good environmental protection effect, reasonable process design, and easy availability of raw materials

Inactive Publication Date: 2018-02-23
TLC NANJING PHARMA RANDD CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The synthesis of anagrelide derivatives and related pharmacology and pharmacokinetic studies on anagrelide derivatives can provide test samples for anagrelide research and quality testing, and anagrelide derivatives also have good Medicinal prospects, but there is no report on the synthetic method of anagrelide derivatives

Method used

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  • Preparation method of anagrelide derivative
  • Preparation method of anagrelide derivative
  • Preparation method of anagrelide derivative

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Embodiment Construction

[0023] Preparation of Compound II: Suspend 1,2,3,4-tetrachlorobenzene in 40mL 98% concentrated sulfuric acid, add a mixed solution of 65% concentrated nitric acid and 9.17mL 98% concentrated sulfuric acid at a certain After stirring at high temperature for 3 hours, the reaction solution changed from a white suspension to a yellow suspension. Pour the reaction solution directly into 200g of ice, add 200mL of water, extract twice with 200mL of ethyl acetate, combine the organic phases, wash with 200mL of water, then wash with 200mL of saturated sodium bicarbonate, dry the organic phase, and evaporate to dryness The ratio of the amount of yellow solid compound II, 1,2,3,4-tetrachlorobenzene to concentrated nitric acid, and the experimental data of the reaction solvent are as follows:

[0024]

[0025] The screening experiment data of optimal reaction temperature are as follows:

[0026]

[0027] Preparation of Compound III: Dissolve 0.07 mol of Compound II in 9.6 mL of sol...

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Abstract

The invention discloses a preparation method of an anagrelide derivative, and belongs to the field of pharmaceutical synthesis. The method is reasonable in process design, high in operability, relatively mild in reaction condition and high in yield, and can realize industrial production. According to the preparation method of the anagrelide derivative, synthesis of the anagrelide derivative is realized by taking 1,2,3,4-tetrachlorobenzene as a raw material through six-step reaction. The anagrelide derivative prepared through the preparation method provides an important basis for scientific evaluation of the quality, the safety and the efficacy of anagrelide; furthermore, the anagrelide derivative is high in pharmacological activity, can be prepared into drugs for treating thrombocytosis caused by various reasons, and has an important application value.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a preparation method of anagrelide derivatives. Background technique [0002] Platelet aggregation inhibitor Anagrelide is an oral anti-platelet aggregation drug, a cyclophosphine (cMAP) phosphodiacylase (PDE) inhibitor, chemical name 6,7-dichloro-l,2,3,5 -Tetrahydroimidazo[2,1-b]quinazolin-2-(3H)-one, trade name Agrylin, was developed by Roberts Phnaajeeutieals in the United States, and was approved to be listed in the United States in July 1997. The drug has the advantages of strong selectivity, no leukopenia, anemia, and serious side effects of leukemia. At present, it is used to treat thrombocytosis caused by essential thrombocythemia and myeloproliferative diseases, which can reduce the number of platelets in patients by 50% within a week, and the effective rate is over 80%. It can even treat patients who are ineffective after hydroxyurea treatment. Within the therapeutic dos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 吴文超徐庶张池崔希林
Owner TLC NANJING PHARMA RANDD CO LTD
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