EnamineStore Blog

Apalutamide Retrosynthesis

Apalutamide (Erleada™, Janssen Biotech, Inc.) is an oral androgen receptor (AR) inhibitor which was approved by FDA for patients with non-metastatic castration-resistant prostate cancer (NM-CRPC) on February 14, 2018.

Synthesis of this small molecule may be realized starting from these Building Blocks:

Apalutamide retrosynthesis

 

Here are some analogs and similar Building Blocks, available from stock:

2-bromo-3-trifluoromethylpyridine 6-chloro-5-(trifluoromethyl)pyridin-3-amine 5-bromo-2-chloro-3-(trifluoromethyl)pyridine 2,5-dichloro-3-(trifluoromethyl)pyridine 2-chloro-5-nitro-3-(trifluoromethyl)pyridine 2-Chloro-3-(trifluoromethyl)pyridine 6-chloro-5-(trifluoromethyl)pyridine-3-sulfonamide 6-chloro-5-(trifluoromethyl)pyridine-3-sulfonyl chloride methyl 6-chloro-5-(trifluoromethyl)pyridine-3-carboxylate3,3-dimethylcyclobutan-1-one spiro[2.3]hexan-5-one spiro[3.3]heptan-2-one spiro[3.4]octan-2-one spiro[3.5]nonan-2-one 3-cyclobutylcyclobutan-1-one 3-tert-butylcyclobutan-1-one 3-(propan-2-yl)cyclobutan-1-one 3-ethylcyclobutan-1-one 3-methylcyclobutan-1-one cyclobutanone 3,3-difluorocyclobutan-1-one 3-(difluoromethyl)cyclobutan-1-one 3,3-bis(fluoromethyl)cyclobutan-1-one 6,6-difluorospiro[3.3]heptan-2-one 2-cyclopropylcyclobutan-1-one 2-tert-butylcyclobutan-1-one 2-(propan-2-yl)cyclobutan-1-one 2-ethylcyclobutan-1-one 2-methylcyclobutan-1-one 2,2-dimethylcyclobutan-1-one 2,3-dimethylcyclobutan-1-one spiro[3.3]heptan-1-one spiro[3.4]octan-1-one 2,2,4,4-tetramethylcyclobutan-1-onemethyl 4-amino-2-chloro-6-fluorobenzoate 4-amino-2,5-difluorobenzoic acid 4-amino-2-fluorobenzoic acid methyl 4-amino-2-fluorobenzoate hydrochloride methyl 4-amino-2-fluoro-6-methylbenzoate hydrochloride 2-bromo-6-fluoro-4-nitrobenzoic acid 2,5-DIFLUORO-4-NITROBENZOIC ACID 2-fluoro-4-nitrobenzoic acid methyl 2-fluoro-4-nitrobenzoate 4-amino-2-fluoro-5-methylbenzoic acid hydrochloride 4-amino-2-fluoro-5-methyl-benzoic acid methyl ester methyl 4-amino-2,6-difluorobenzoate 4-amino-2,6-difluorobenzoic acid methyl 4-amino-5-chloro-2-fluorobenzoate 4-amino-5-chloro-2-fluorobenzoic acid