- Synthesis method of relugolix or salt thereof
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The invention provides a synthesis method of relugolix or a salt thereof, wherein thesynthesis method comprises the steps: taking 1-(dimethylamino)-3-(4-nitrophenyl)-2-acetone and cyanoacetate as initial raw materials, and carrying out condensation cyclization, alkylation reaction, Ullmann reaction and coupling reaction to obtain a relugolix 4 free alkali form or salt form. The synthetic route optimized the process, the route steps are shortened, the route efficiency is improved, the use of noble metal catalysts can be reduced, and the process cost is greatly reduced. The route is simple to operate, the total yield is high, the purity of the obtained product is high, and the method is suitable for large-scale production. The forms of the three salts of relugolix are also found, the crystallinity is good, the purification is easy, and the product purity is favorably improved.
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- Preparation method of Relugolix and intermediate compounds
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The invention provides a novel preparation method of Relugolix and two novel intermediate compounds. The preparation method comprises the following steps: reducing an existing compound 2 to obtain an amino compound 3, then, carrying out a condensation rea
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Paragraph 0105-0106
(2021/05/05)
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- Five-membered nitrogen-containing heteroaryl substituted pyrimidinedione compound and application thereof
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The invention belongs to the technical field of medicines, and relates to a five-membered nitrogen-containing heteroaryl substituted pyrimidinedione compound and application thereof, and a pharmaceutical composition containing the five-membered nitrogen-containing heteroaryl substituted pyrimidinedione compound, and the five-membered nitrogen-containing heteroaryl substituted pyrimidinedione compound and the pharmaceutical composition can be used as gonadotropin releasing hormone receptor antagonists. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis, hysteromyoma, precocious puberty and the like.
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- Nitrogen-containing heterocyclic group substituted pyrimidinedione compound and application thereof
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The invention belongs to the technical field of medicines, and relates to a nitrogen-containing heterocyclic group substituted pyrimidinedione compound and application thereof, and a pharmaceutical composition containing the compound, which can be used as a gonadotropin releasing hormone receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis,hysteromyoma, precocious puberty and the like.
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- Bicyclic nitrogen-containing heteroaryl substituted pyrimidinedione compounds and application thereof
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The invention belongs to the technical field of medicines, and relates to bicyclic nitrogen-containing heteroaryl substituted pyrimidinedione compounds, application thereof, and a pharmaceutical composition containing the compounds. The compounds can be used as a gonadotropin releasing hormone receptor antagonist. The invention also relates to a method for preparing the compounds and the pharmaceutical composition, and application of the compounds and the pharmaceutical composition in prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis, hysteromyoma, precocious puberty and the like.
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- Substituted pyrimidinedione compound and application thereof
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The invention belongs to the technical field of medicines, and relates to a substituted pyrimidinedione compound and application thereof, and a pharmaceutical composition containing the compound, which can be used as a gonadotropin releasing hormone receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis, hysteromyoma, precocious puberty and the like.
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