875548-97-3Relevant academic research and scientific papers
Pd-Catalysed direct C(sp2)-H fluorination of aromatic ketones: Concise access to anacetrapib
Wu, Qiuzi,Mao, Yang-Jie,Zhou, Kun,Wang, Shuang,Chen, Lei,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
, p. 4544 - 4547 (2021/05/17)
The Pd-cataylsed direct ortho-C(sp2)-H fluorination of aromatic ketones has been developed for the first time. The reaction features good regioselectivity and simple operations, constituting an alternative shortcut to access fluorinated ketones. A concise synthesis of anacetrapib has also been achieved by using late-stage C-H fluorination as a key step.
Anacetrapib key intermediate as well as synthesis method and application thereof
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Paragraph 0098; 0118-0121, (2021/06/21)
The invention provides a synthesis method of an Anacetrapib key intermediate (a compound shown in a formula H). According to the method, all starting raw materials are simple and easy to obtain, and synthesis steps can be shortened. The method is short in route; initial raw materials are easy to obtain, and the overall reaction yield is high; and the reaction route is simple in post-treatment and few in reaction by-products.
Preparation method of Anacetrapib
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, (2017/07/20)
The invention relates to a preparation method of a compound represented by the formula (I). The preparation method comprises the following steps: (1) reacting 2-chloro-5-trifluoromethyl-aniline (II) with (4-fluoro-5-isopropyl-2-methoxyphenyl)boric acid (III) to obtain 2-(4-fluoro-5-isopropyl-20methoxyphenyl)-5-trifluoromethyl-aniline (formula IV); (2) reacting the compound (formula IV) with tert-butyl nitrite, acetaldehyde, and alkalis to obtain 2-(4-fluoro-5-isopropyl-2-methoxyphenyl)-5-trifluoromethyl-benzyl alcohol (formula V); (3) reacting the compound (formula V) with a halogenation reagent, and then adding (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidine-2-one (VI) into the reaction mixture to carry out reactions so as to obtain (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-{[4'-fluoro-5'-isoproypyl-2'-methoxy-4-(trifluoromethyl)biphenyl-2-yl]methyl}-4-methyl-1,3-oxazolidine-2-one represented by the formula (I), namely Anacetrapib.
Process for a CETP Inhibitor
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, (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 PREPARATION OF ANACETRAPIB AND INTERMEDIATES THEREOF
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Page/Page column 24, (2014/08/06)
The present invention relates to a novel process for the preparation of anacetrapib. The present invention also relates to novel intermediate or its salt and its use in the preparation of anacetrapib.
SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF
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Page/Page column 44-45, (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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, (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:.
COMPOUNDS FOR INCREASE OF HDL-C LEVEL AND USES THEREOF
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Page/Page column 17, (2012/04/17)
Compounds for inhibiting cholesterol ester transport protein (CETP) activity and application thereof. These compounds include compounds of formula (I), and the pharmaceutically acceptable salts, solvates, non-covalent complexes,chelates, or prodrugs there
Synthesis of intermediates for preparing anacetrapib and derivates thereof
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, (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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, (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.
