- Novel synthetic method for (4-fluoro-5-isopropyl-methoxyphenyl)boric acid
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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
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- Preparation method of Anacetrapib key intermediate
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The invention relates to a preparation method of an Anacetrapib key intermediate 1-bromo-4-fluoro-5-isopropyl-2-methoxybenzene. The preparation method comprises the following steps: hydrolyzing an initial raw material 2,4-difluoronitrobenzene to obtain 4-fluoro-2-hydroxynitrobenzene, methylating 4-fluoro-2-hydroxynitrobenzene to obtain 4-fluoro-2-methoxynitrobenzene, carrying out nitro group reduction to form 4-fluoro-2-methoxyaniline, carrying out diazo bromination to obtain 4-fluoro-2-methoxybromobenzene, carrying out Friedel-Crafts acylation to obtain 2-fluoro-4-methoxy-5-bromoacetophenone, carrying out a condensation reaction to obtain 2-(2-fluoro-4-methoxy-5-bromophenyl)-propane-2-ol, carrying out an elimination reaction to obtain 1-bromo-4-fluoro-2-methoxy-5-(1-methylvinyl)benzene, and hydrogenating the 1-bromo-4-fluoro-2-methoxy-5-(1-methylvinyl)benzene to obtain 1-bromo-4-fluoro-5-isopropyl-2-methoxybenzene. The preparation method has the advantages of realization of low cost, good quality and high yield of the above final product, mild reaction conditions, simplicity in operation, and easiness in industrialization.
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- Process for a CETP Inhibitor
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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:
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- SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF
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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.
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Page/Page column 41
(2013/07/05)
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- PROCESS FOR A CETP INHIBITOR
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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:.
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- Synthesis of intermediates for preparing anacetrapib and derivates thereof
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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.
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Page/Page column 34
(2012/07/03)
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- Synthesis of intermediates for preparing anacetrapib and derivates thereof
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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.
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- SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF
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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.
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- Preparative scale synthesis of the biaryl core of anacetrapib via a ruthenium-catalyzed direct arylation reaction: Unexpected effect of solvent impurity on the arylation reaction
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In this report, we disclose our findings regarding the remarkable effect of a low-level impurity found in the solvent used for a ruthenium-catalyzed direct arylation reaction. This discovery allowed for the development of a robust and high-yield arylation protocol that was demonstrated on a multikilogram scale using carboxylate as the cocatalyst. Finally, a practical, scalable, and chromatography-free synthesis of the biaryl core of Anacetrapib is described.(Figure Presented)
- Ouellet, Stephane G.,Roy, Amelie,Molinaro, Carmela,Angelaud, Remy,Marcoux, Jean-Francois,OShea, Paul D.,Davies, Ian W.
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p. 1436 - 1439
(2011/04/26)
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- PROCESS FOR SYNTHESIZING A CETP INHIBITOR
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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.
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Page/Page column 7-8
(2010/11/25)
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- POLYMER FORMULATIONS OF CETP INHIBITORS
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A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer; and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol.
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Page/Page column 20
(2010/11/28)
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