- Preparation method of (R)-bicalutamide intermediate
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The invention relates to a method for preparing an (R)-bicalutamide intermediate. The method comprises the following steps: taking methacrylic acid as a raw material, and obtaining the (R)-bicalutamide intermediate through several steps of esterification, hydroxylation and sulfonation, namely, (R)-3-(4-fluorophenylsulfydryl)-2-hydroxy-2-methylpropionic acid. (R)-bicalutamide with enantioselectivity of more than 99% can be obtained by two simple follow-up reactions of the intermediate. The preparation method has the advantages of easily available starting materials, high reaction yield, easy operation in reaction, high enantioselectivity and wide industrial application prospects.
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Paragraph 0051; 0061-0063
(2021/04/21)
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- ANDROGEN RECEPTOR ANTAGONISTS
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Disclosed herein are compositions and methods for modulating the androgen receptor.
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Paragraph 0325
(2016/04/26)
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- SELECTIVE ANDROGEN RECEPTOR MODULATORS, ANALOGS AND DERIVATIVES THEREOF AND USES THEREOF
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This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including,inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.
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Page/Page column 139; 140; Sheet 6
(2008/06/13)
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- Syntheses of enantiomerically pure (R)- and (S)-bicalutamide
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The racemic antiandrogen bicalutamide is the leading antiandrogen used for the treatment of prostate cancer. The (R)-isomer possesses virtually all of the activity, but both isomers are metabolized by the liver. A convenient synthetic route to the active enantiomer would be an attractive option for patients who are hepatically impaired. We now demonstrate a rather short synthesis of (R)-bicalutamide, starting with a naturally occurring, chiral precursor.
- James, Kenneth D,Ekwuribe, Nnochiri N
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p. 5905 - 5908
(2007/10/03)
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