915087-25-1

Basic information

• Product Name: 4-AMINO-2-FLUORO-N-METHYLBENZAMIDE
• Synonyms: 4-AMINO-2-FLUORO-N-METHYLBENZAMIDE;N-Methyl-2-fluoro-4-aminobenzamide;BenzaMide, 4-aMino-2-fluoro-N-Methyl-;2. 4-aMino-2-fluoro-N-MethylbenzaMide;N-Methyl-4-amino-2-fluoro-benzamide;4-amino-2-fluoro-N-menthylbenzamide
• CAS NO: 915087-25-1
• Molecular Formula: C₈H₉FN₂O
• Molecular Weight: 168.17
• Mol File: 915087-25-1.mol
• Article Data: 19

Chemical Properties

• Boiling Point: 320℃
• Flash Point: 147℃
• Appearance: /
• Density: 1.234
• Storage Temp.: Keep in dark place,Inert atmosphere,Room temperature
• Solubility: Chloroform (Slightly), Methanol (Slightly)
• PKA: 14.12±0.46(Predicted)
• Stability: Moisture Sensitive
• CAS DataBase Reference: 4-AMINO-2-FLUORO-N-METHYLBENZAMIDE(CAS DataBase Reference)
• NIST Chemistry Reference: 4-AMINO-2-FLUORO-N-METHYLBENZAMIDE(915087-25-1)
• EPA Substance Registry System: 4-AMINO-2-FLUORO-N-METHYLBENZAMIDE(915087-25-1)

Safety Data

• Hazardous Substances Data: 915087-25-1(Hazardous Substances Data)

Usage

Uses

4-?Amino-?2-?fluoro-?N-?methylbenzamide acts as a reagent in the design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists. Also, in the preparation and structure-activity relationship of chiral benzyloxypyridinone derivatives as c-Met kinase inhibitors

InChI:InChI=1S/C8H9FN2O/c1-11-8(12)6-3-2-5(10)4-7(6)9/h2-4H,10H2,1H3,(H,11,12)

Upstream product

• 915087-24-0 2-fluoro-N-methyl-4-nitro-benzamide 
• 74-89-5 methylamine 
• 948717-18-8 2,4-difluoro-N-methylbenzamide 
• 72482-64-5 2,4-difluorobenzoyl chloride 
• 1427-07-2 2-fluoro-4-nitrotoluene 
• 403-24-7 2-fluoro-4-nitrobenzoic acid 
• 956104-46-4 2-fluoro-4-(4-methoxybenzylamino)-N-methylbenzamide 

Downstream Products

• 915087-26-2 4-(1-cyano-cyclobutanylamino)-2-fluoro-N-methyl-benzamide 
• 915087-32-0 N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide 
• 1245736-64-4 4-[7-(2-chloro-4-cyano-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1245736-42-8 4-[7-(4-cyano-3-methoxy-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1272718-96-3 4-[7-(4-cyano-2,5-difluoro-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1245736-60-0 4-[7-(4-cyano-2-trifluoromethoxy-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1245736-61-1 4-[7-(4-cyano-2-fluoro-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1245736-62-2 4-[7-(4-cyano-2-methyl-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1245736-63-3 4-[7-(4-cyano-2-trifluoromethyl-phenyl)-8-oxo-6-thio-5,7-diazaspiro[3,4]-5-octyl]-2-fluoro-N-methyl benzamide 
• 1272718-97-4 4-[7-(3-chloro-4-cyano-2-fluoro-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1245736-43-9 4-[7-(3,4-dicyano-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1272718-98-5 4-[7-(4-cyano-2-fluoro-3-trifluoromethyl-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide 
• 1272718-99-6 4-[3-(3-chloro-4-cyano-2-fluoro-phenyl)-5,5-dimethyl-4-oxo-2-thioxo-imidazolidin-1-yl]-2-fluoro-N-methyl-benzamide 
• 1272719-00-2 4-[3-(4-cyano-2-fluoro-3-trifluoromethyl-phenyl)-5,5-dimethyl-4-oxo-2-thioxo-imidazolidin-1-yl]-2-fluoro-N-methyl-benzamide 

Relevant articles and documents

Process for the preparation of 4-[7-(6-Cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7- diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide and its polymorphs

The present application relates a process for the preparation of 4- [7 - (6-Cyano- 5- trifluoro methyl pyridin-3- yl) -8- oxo -6- thioxo- 5,7- diazaspiro [3.4] oct-5- yl]- 2-fluoro-N-methyl benzamide of formula-1. The present application further discloses a processes for the preparation of amorphous and crystalline form of compound of formula-1. Formula-1.

SOLID STATE FORMS OF APALUTAMIDE

Disclosed are solid state forms of Apalutamide and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof.

Effect of N-methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide

Enzalutamide, a second-generation antiandrogen, has been developed for the treatment of castration-resistance prostate cancer. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger antitumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.