22902-87-0Relevant articles and documents
A 2-halo-5-trifluoromethylbenzoate methyl animal pen alcoholic compound preparation method
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Paragraph 0038-0041, (2017/02/09)
The invention relates to the field of a medical intermediate, and particularly discloses a preparation method of intermediate 2-halogenate-5-trifluoromethyl benzyl alcohol of a novel cholesterol-lowering medicament, namely a cholesteryl ester transfer protein (CETP) inhibitor. The method comprises the following steps: carrying out chloromethylation reaction and esterification reaction on 4-halogenated trifluorotoluene used as a raw material, and then carrying out hydrolysis reaction so as to obtain a product 2-halogenate-5-trifluoromethyl benzyl alcohol compound. The method disclosed by the invention is available in raw materials, low in cost, environment-friendly and energy-saving, simple in process, easy for realization of industrialization, high in product yield, good in purity and stable in quality, and completely accords with the operating requirements on the medical intermediate.
Synthesis of stable isotope labeled anacetrapib, its major metabolites and [14C]anacetrapib
Kuethe, Jeffrey T.,Soli, Eric D.,Royster, Pernilla,Quinn, Catherine A.
, p. 600 - 608 (2013/12/04)
Cholesteryl ester transfer protein inhibitors are an important class of compounds designed to treat hypocholesterolemia and prevent cardiovascular disease. Anacetrapib (MK-0859) is currently in phase III trials for the treatment of elevated cholesterol levels and prevention of cardiovascular disease. In order to further support the development of anacetrapib, we prepared [M + 6]MK-0859, which was required in support of an absolute bioavailability study of the active pharmaceutical ingredient (API). Additional support included the synthesis of an internal standard [M + 13] and three stable isotope labeled metabolites, which were used to analyze clinical samples, and [ 14C]MK-0859 to support drug metabolism studies. A labeling strategy for the preparation of [M + 6], [M + 13], and [14C]anacetrapib is described. The preparation of stable isotope labelled metabolites of anacetrapib is also described.