875446-29-0Relevant articles and documents
Preparation method of anacetrapib intermediate
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Paragraph 0026; 0027; 0028; 0029; 0030; 0031-0052, (2019/03/10)
The invention relates to a preparation method of an anacetrapib intermediate, namely (4-fluoro-5-isopropyl-2-methoxyphenyl) boric acid. According to the preparation method, 4-fluoro-1-bromo-2-methoxyl-5-isopropyl benzene and triisopropyl borate carry out reactions under the action of a catalyst to prepare (4-fluoro-5-isopropyl-2-methoxyphenyl) boric acid. A novel catalyst is adopted, the novel catalyst can be diisopropyl magnesium lithium chloride (i-Pr2Mg LiCl), 2,2',6,6'-tetramethyl piperidine magnesium chloride lithium chloride (TMP MgCl LiCl), or 2,4,6-trimethylphenyl magnesium bromide lithium chloride (Mes MgBr LiCl). The reaction conditions are mild; the reaction speed is quick; the product is single; the purification is convenient; the purity and yield of obtained intermediate are high, and the preparation method is suitable for industrial production.
Process for a CETP Inhibitor
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Paragraph 0041; 0042; 0043, (2014/10/16)
An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:
PROCESS FOR A CETP INHIBITOR
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Page/Page column 8, (2013/05/22)
An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:.