627484-44-0Relevant articles and documents
Preparation method of bicalutamide intermediate
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Paragraph 0015; 0016; 0017; 0018; 0019; 0020; 0021, (2017/07/20)
The invention provides a preparation method of a bicalutamide intermediate, and in particular relates to a method of preparing 3-chloro-N-(4-cyano-3-trifluromethyl phenyl)-2-hydroxyl-2-methyl propanamide by using N-(4-cyano-3-trifluromethyl phenyl) methacrylamide. The method comprises the following steps: in a solvent, by taking N-(4-cyano-3-trifluromethyl phenyl) methacrylamide as a raw material, adding an acid; cooling the solution to 0-15 DEG C; stirring the mixture; dropwise adding a sodium hypochlorite solution to oxidize; after dropwise addition, keeping the temperature of a reaction system at 0-15 DEG C to perform a reaction for 0.5-1h; and separating and purifying the obtained solution to obtain high-purity 3-chloro-N-(4-cyano-3-trifluromethyl phenyl)-2-hydroxyl-2-methyl propanamide. The preparation method is safe and economical and can be suitable for preparing bicathioether intermediates on a large scale. The raw material is cheap and is easily available, the production period is shortened, and the environmental pollution is not generated.
Novel pathway for the synthesis of arylpropionamide-derived selective androgen receptor modulator (SARM) metabolites of andarine and ostarine
Schragl, Katharina M.,Forsdahl, Guro,Gmeiner, Guenter,Enev, Valentin S.,Gaertner, Peter
supporting information, p. 2239 - 2242 (2013/05/09)
O-Dephenylandarine and O-dephenylostarine, two SARM metabolites relevant for doping control analysis, were synthesized in their endogenous (S)-forms as well as in terms of their racemates. The enantiopure (S)-metabolites were obtained after six steps in 20% and 23% overall yield, the slightly modified racemic route provided the compounds in 28% and 31% total yield, respectively.