830346-46-8Relevant academic research and scientific papers
Preparation method of olagolide intermediate
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Paragraph 0036-0039; 0044-0048, (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
Ammonium Chloride-Promoted Rapid Synthesis of Monosubstituted Ureas under Microwave Irradiation
Lan, Chunling Blue,Auclair, Karine
supporting information, p. 5135 - 5146 (2021/10/19)
Monosubstituted ureas are important scaffolds in organic chemistry. They appear in various biologically active compounds and serve as versatile precursors in synthesis. Monosubstituted ureas were originally prepared using toxic and hazardous phosgene equivalents. Modern methods include transamidation of urea and nucleophilic addition to cyanate salts, both of which suffer from a narrow substrate scope due to the need for a strong acid and prolonged reaction times. We hereby report that ammonium chloride can promote the reaction between amines and potassium cyanate to generate monosubstituted ureas in water. This method proceeds rapidly under microwave irradiation and tolerates a broad range of functional groups. Unlike previous strategies, it is compatible with other nucleophiles, acid-labile moieties, and most of the common protecting groups. The products precipitate out of solution, allowing facile isolation without column chromatography.
Preparation method of oxlagrel intermediate
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Paragraph 0047-0054, (2020/12/10)
The invention relates to a preparation method of an oxlagrel intermediate. The preparation method comprises the following steps: dissolving a 2-fluoro-6-(trifluoromethyl)benzyl bromide compound 7 in an aprotic polar solvent, then adding alkali carbonate and urea, carrying out a heating reaction under stirring, and after the reaction is finished, carrying out post-treatment and recrystallization toobtain a compound 4, the yield being 89-95 wt%; and dissolving the compound 4 prepared in the step (1) into the aprotic polar solvent; then, adding a 2-bromoacetoacetic acid ethyl ester compound 9, and cooling to 3 DEG C or below, adding bromo-organosilane while stirring, then continuing to stir and react at 80 DEG C or below, and after the reaction is finished, carrying out aftertreatment and recrystallization to obtain the target product 5-bromo-1-(2-fluoro-6-trifluoromethylbenzyl)-6-methylpyrimidine (1H, 3H)-2,4-diketone compound 1, the yield being 75-88 wt%. The method is simple in synthetic route and simple and convenient in post-treatment mode.
Preparation method of 1-(2-fluoro-6-(trifluoromethyl)benzyl)urea
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Paragraph 0031; 0033-0034, (2020/07/12)
The invention discloses a preparation method of 1-(2-fluoro-6-(trifluoromethyl)benzyl)urea. The preparation method comprises the following steps: reducing a compound 2-fluoro-6-(trifluorophenyl)cyanophenyl into a compound (2-fluoro-6-(trifluoromethyl)benzyl)tert-butyl carbamate through a reducing agent under the condition that a catalyst and di-tert-butyl dicarbonate participate; and then reactingthe compound (2-fluoro-6-(trifluoromethyl)benzyl)tert-butyl carbamate with urea in a hydrochloric acid solution to obtain a key intermediate compound 1-(2-fluoro-6-(trifluoromethyl)benzyl)urea of elagolix. The method has the beneficial effects of avoidance of the use of toxic reagents, mild reaction conditions, low cost, high yield, simplified route, and suitability for industrial large-scale production.
Elagolix Sodium Compositions and Processes
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Paragraph 0426, (2020/02/13)
The present invention relates to compositions of elagolix sodium, and process and intermediates for the preparation thereof.
Substituted pyrimidine-2, 4(1H, 3H)-dione derivative and uses thereof
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Paragraph 0138; 0143-0147, (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 C13H10F4N2O2
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Page/Page column 4-7, (2020/04/17)
The invention discloses a preparation method of C13H10F4N2O2 and relates to the field of compound production. The preparation method includes: S1, adding urea to distilled water to prepare a mixture IM C, and adding the mixture IM C to a reaction kettle a
Method for preparing intermediate of elagolix
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, (2019/12/09)
The invention relates to a method for preparing an intermediate of elagolix. In particular, the invention discloses a method for preparing a key intermediate compound E8 of elagolix, and compounds such as a compound E4 for preparing the intermediate compound E8. The method is simple and convenient in operation, mild in condition and very applicable to industrial production.
Method for preparing agomelatine intermediate (by machine translation)
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, (2019/12/09)
The invention relates to a method for preparing an intermediate of agomelatine. The method is simple and convenient to E8 operate, mild E8 in condition and very suitable for industrial production C. (by machine translation)
Method for preparing GnRHR drug key intermediate compound
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Paragraph 0041; 0049-0053; 0060-0063; 0070-0072, (2019/08/07)
The invention discloses a method for preparing a GnRHR drug key intermediate compound. According to the invention, a synthetic route of the GnRHR drug key intermediate is changed, and meanwhile, a boron hydrogen salt is taken as a reducing agent and a chl
