5773-80-8Relevant articles and documents
Ruthenium-catalyzed ester reductions applied to pharmaceutical intermediates
Shaalan, Youssef,Boulton, Lee,Jamieson, Craig
supporting information, p. 2745 - 2751 (2020/11/30)
Ruthenium pincer complexes were synthesized and used for catalytic ester reductions under mild conditions (~5 bar of hydrogen). An experimental design approach was used to optimize the conditions for yield, purity, and robustness. Evidence for the catalytically active ruthenium dihydride species is presented. Observed intermediates and side products, as well as time-course data, were used to build mechanistic insight. The optimized procedure was further demonstrated through scaled-up reductions of two pharmaceutically relevant esters, both in batch and continuous flow.
BIARYL DERIVATIVE AS GPR120 AGONIST
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Paragraph 0306, (2017/11/17)
The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
Process for synthesizing 6-bromo-2-naphthol
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Paragraph 0035, (2017/05/23)
The invention relates to a process for synthesizing 6-bromo-2-naphthol. The process comprises the following steps: (S1) mixing 2-naphthol and a bromo salt, and adding the mixture into a reactor; (S2) adding an acetic solution into the reactor in the step (S1); (S3) dropwise adding an oxidant into the reactor while carrying out stirring, and carrying out a heat-insulating reaction after dropwise adding is completed, so as to obtain an intermediate solution; (S4) heating the temperature of the reactor to a definite value, adding nano Pd/Fe into the intermediate solution obtained in the step (S3), introducing nitrogen gas into the reactor, and carrying out a reaction while controlling the temperature and pressure to definite values; (S5) cooling the reactor, adding pure water into the reactor in the step (S4) for dilution, and carrying out standing for a period of time for crystallization; and (S6) subjecting the crystals obtained in the step (S5) to filtering and washing, adding the crystals into an acetic solution for recrystallization, and subjecting the recrystallized crystals to filtering, washing and drying, thereby obtaining a finished product. According to the process, on one hand, the utilization ratio of atoms is increased, and large-area pollution to environments caused by reactions is prevented; and on the other hand, the requirements of a reaction process on public works are relatively low, the reaction rate is relatively high, and the purity and yield of the obtained final product are relatively high, so that the process is applicable to industrial mass production.