830346-47-9Relevant academic research and scientific papers
Preparation method of olagolide intermediate
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Paragraph 0036-0037; 0040-0041; 0044-0045; 0049-0050, (2022/01/12)
The present invention relates to a method for preparing a lacolagoli intermediate 5-bromo-1- {[2-fluoro-6-(trifluoromethyl)phenyl] methyl}-6-methyl-2,4 (1H, 3H) pyrimidinedione (compound of formula I), in particular, a compound of formula III with 2-fluor
Preparation method of elagolix intermediate
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, (2021/01/25)
The invention relates to a preparation method of an elagolix intermediate 1-(2-fluoro-6-trifluoromethylphenyl)-6-methyl pyrimidine-2,4(1H,3H)-diketone (I). The method comprises the following steps: taking 1-(2-fluoro-6-trifluoromethylphenyl)urea (V) and acetacetate (IV) protected by ketal as raw materials, reacting in the presence of alkali to obtain a ketal intermediate (III), and converting theketal intermediate (III) into N-((2-fluoro-6-trifluoromethylphenyl)carbamoyl)-3-oxobutylamide (II); and finally, carrying out a ring closing reaction to obtain the elagolix intermediate 1-(2-fluoro-6-trifluoromethylphenyl)-6-methyl pyrimidine-2,4(1H,3H)-diketone (I). According to the invention, the initial raw materials are cheap and easily available, and ketal-protected acetoacetate (IV) is usedas the raw material, so that the generation of isomers is avoided, and the product quality is improved.
AN IMPROVED PROCESS FOR THE PREPARATION OF 4-({(1 R)-2-[5-(2-FLUORO-3METHOXYPHENYL)-3-{[2-FLUORO-6-(TRIFLUORO METHYL) PHENYL]METHYL}-4-METHYL-2,6-DIOXO-3,6DIHYDROPYRIMIDIN-1(2 H)-YL]-1-PHENYLETHYL}AMINO)BUTANOIC ACID OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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, (2021/07/02)
The present invention relates to an improved process for the preparation of 4- ({(1R) -2- [5- (2-fluoro- 3- methoxy phenyl) – 3 - {[ 2-fluoro- 6-(trifluoro methyl) phenyl] methyl} -4-methyl- 2,6-dioxo- 3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl}amino) butanoic acid of formula (I) or its pharmaceutically acceptable salts. The compound of formula (I) is represented by the following structural formula.
METHOD FOR PREPARING ELAGOLIX INTERMEDIATE AND COMPOSITION THEREOF
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, (2020/12/08)
The present invention relates to a method for preparing an intermediate (Formula IV) of sodium elagolix. The intermediate is prepared by the following route. The method has advantages of simple and safe operation, high yield, less environmental pollution, good economic effect and suitability for industrial production, wherein R represents C1-C4 substituted or unsubstituted benzyl or allyl.
Preparation method of compound containing 6-methyluracil structure
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Paragraph 0038; 0047-0052; 0054; 0058-0059; 0060; 0064-0065, (2020/07/12)
The invention discloses a preparation method of a compound containing a 6-methyluracil structure. The invention relates to the technical field of synthesis of medical intermediates and organic chemical intermediates. The method comprises the following synthesis steps of: (1) reacting ethyl carbamate serving as a compound 1 with ethyl acetoacetate serving as a compound 2 under a heating condition under the action of an organic solvent and a catalyst to generate a compound 3 that is oxazine diketone; and (2) reacting the compound 3 with a compound 4 that is 2-fluoro-6-(trifluoromethyl) phenyl) methylamine under the condition of heating, an organic solvent or no solvent to generate a compound 5, i.e., a 6-methyl-uracil substituted derivative. The method disclosed by the invention is suitablefor industrial production and relatively low in cost, and the prepared product is high in purity and yield.
Elagolix intermediate preparation method
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Paragraph 0016; 0017, (2020/01/25)
The invention discloses an elagolix intermediate preparation method, which specially comprises: 1, preparing 1-fluoro-2-(iodomethyl)-3-(trifluoromethyl)benzene from 2-trifluoromethyl-6-fluorobenzaldehyde, an iodinating reagent and a mixed solvent under th
Substituted pyrimidine-2, 4(1H, 3H)-dione derivative and uses thereof
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Paragraph 0138; 0143; 0148-0151, (2020/07/12)
The invention belongs to the technical field of medicines, and relates to a substituted pyrimidine-2, 4(1H, 3H)-dione derivative and uses thereof, and a pharmaceutical composition containing the compound. The derivative 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 uses 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.
Preparation method of elagolix intermediate
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Paragraph 0026-0053; 0062-0071, (2019/10/02)
The invention relates to a preparation method of an elagolix intermediate (IV). The method is carried out according to the following route, and the synthetic route is short. The method has the advantages of simple and safe operation, good yield, small env
Method for synthesizing Elagolix midbody polysubstituted pyrimidine derivate through two-step method
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Page/Page column 6-10, (2019/06/11)
The invention discloses a method for synthesizing an Elagolix midbody polysubstituted pyrimidine derivate through a two-step method. The method comprises the following steps that (1) (2-fluoro-6-(trifluoromethyl)phenyl)methylamine shown as a formula II re
PROCESSES TO PRODUCE ELAGOLIX
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Page/Page column 13; 14, (2019/06/23)
The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.
