875446-29-0Relevant academic research and scientific papers
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.
Novel synthetic method for (4-fluoro-5-isopropyl-methoxyphenyl)boric acid
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Paragraph 0025; 0032; 0037, (2018/04/01)
The invention discloses a novel synthetic method for (4-fluoro-5-isopropyl-methoxyphenyl)boric acid. According to the method, easily available and cheap 2-fluoro-4-methoxyacetophenone is used as a raw material and subjected to a Witting reaction, a hydrog
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:
SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF
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Page/Page column 42, (2013/07/05)
The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
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:.
Synthesis of intermediates for preparing anacetrapib and derivates thereof
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Page/Page column 34-35, (2012/07/03)
The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
Synthesis of intermediates for preparing anacetrapib and derivates thereof
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Page/Page column 36, (2012/07/03)
The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF
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Page/Page column 46, (2012/07/13)
The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: Modifications of the oxazolidinone ring leading to the discovery of anacetrapib
Smith, Cameron J.,Ali, Amjad,Hammond, Milton L.,Li, Hong,Lu, Zhijian,Napolitano, Joann,Taylor, Gayle E.,Thompson, Christopher F.,Anderson, Matt S.,Chen, Ying,Eveland, Suzanne S.,Guo, Qiu,Hyland, Sheryl A.,Milot, Denise P.,Sparrow, Carl P.,Wright, Samuel D.,Cumiskey, Anne-Marie,Latham, Melanie,Peterson, Laurence B.,Rosa, Ray,Pivnichny, James V.,Tong, Xinchun,Xu, Suoyu S.,Sinclair, Peter J.
experimental part, p. 4880 - 4895 (2011/09/20)
The development of the structure-activity studies leading to the discovery of anacetrapib is described. These studies focused on varying the substitution of the oxazolidinone ring of the 5-aryloxazolidinone system. Specifically, it was found that substitution of the 4-position with a methyl group with the cis-stereochemistry relative to the 5-aryl group afforded compounds with increased cholesteryl ester transfer protein (CETP) inhibition potency and a robust in vivo effect on increasing HDL-C levels in transgenic mice expressing cynomolgus monkey CETP.
PROCESS FOR SYNTHESIZING A CETP INHIBITOR
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Page/Page column 7-8, (2010/11/25)
An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.
