335595-52-3

Upstream product

• 371-42-6 4-Fluorothiophenol 
• 261904-39-6 (2R)-3-bromo-2-hydroxy-2-methylpropanoic acid 

Downstream Products

• 890658-79-4 C₁₀H₁₁FO₅S 
• 937802-59-0 bicalutamide 
• 90357-06-5 (R)-bicalutamide 

Relevant academic research and scientific papers

Preparation method of (R)-bicalutamide intermediate

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.

ANDROGEN RECEPTOR ANTAGONISTS

Disclosed herein are compositions and methods for modulating the androgen receptor.

SELECTIVE ANDROGEN RECEPTOR MODULATORS, ANALOGS AND DERIVATIVES THEREOF AND USES THEREOF

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.

Syntheses of enantiomerically pure (R)- and (S)-bicalutamide

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.