915087-24-0

Basic information

• Product Name: 2-FLUORO-N-METHYL-4-NITROBENZAMIDE
• Synonyms: 2-FLUORO-N-METHYL-4-NITROBENZAMIDE;N-Methyl-2-fluoro-4-nitrobenzamide;BenzaMide, 2-fluoro-N-Methyl-4-nitro-;1. 2-fluoro-N-Methyl-4-nitrobenzaMide;4-Nitro-2-fluoro-N-MethylbenzaMide
• CAS NO: 915087-24-0
• Molecular Formula: C₈H₇FN₂O₃
• Molecular Weight: 198.15
• Product Categories: 2-fluoro-N-methyl-4-nitrobenzamide
• Mol File: 915087-24-0.mol

Chemical Properties

• Appearance: /
• Density: 1.358
• Storage Temp.: Sealed in dry,Room Temperature
• CAS DataBase Reference: 2-FLUORO-N-METHYL-4-NITROBENZAMIDE(CAS DataBase Reference)
• NIST Chemistry Reference: 2-FLUORO-N-METHYL-4-NITROBENZAMIDE(915087-24-0)
• EPA Substance Registry System: 2-FLUORO-N-METHYL-4-NITROBENZAMIDE(915087-24-0)

Safety Data

• Hazardous Substances Data: 915087-24-0(Hazardous Substances Data)

Usage

Uses

2-?Fluoro-?N-?methyl-?4-?nitrobenzamide is used in the preparation of androgen receptor antagonists MDV3100. MDV3100 is also a clinical candidate for the treatment of hormone refractory prostrate cancer.

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

• 403-24-7 2-fluoro-4-nitrobenzoic acid 
• 1427-07-2 2-fluoro-4-nitrotoluene 
• 74-89-5 methylamine 
• 593-51-1 methylamine hydrochloride 
• 403-23-6 2-fluoro-4-nitrobenzoyl chloride 

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.

Prostatic cancer treatment medicine

The invention relates to a compound with a prostatic cancer treatment function and nontoxic pharmaceutically acceptable salt of the compound. The structure of the compound is as shown in a formula I,wherein X is C or N, R1 is alkyl of C1-C3 or halogen substituted alkyl, R2 is alkyl of C1-C3 and halogen substituted alkyl or halogen, R3 and R4 are independently selected from H, alkyl and substituted alkyl, and R3 and R4 are connected to form cycloalkyl. The compound has high inhibiting effects on in-situ prostate cancer and transfer of the prostate cancer, and eclamptogenic side effects are lower.

SOLID STATE FORMS OF APALUTAMIDE

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

SUBSTITUTED OXOPYRIDINE DERIVATIVES

The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles

A series of deuterated apalutamide were designed and prepared. Compared to its prototype compound 18, deuterated analogues 19 and 21 showed obviously higher plasma concentrations and better PK parameters after oral administration in mice. In rats, N-trideuteromethyl compound 19 displayed 1.8-fold peak concentration (Cmax), and nearly doubled its drug exposure in plasma (AUC0–∞) compared to compound 18. Unsurprisingly, compounds 18 and 19 had similar affinity for AR in vitro. In summary, the deuteration strategy could obviously improve PK parameters of apalutamide.

SUBSTITUTED OXOPYRIDINE DERIVATIVES

The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and o edemas, and also ophthalmic disorders.

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.

PROCESS FOR THE PREPARATION OF ENZALUTAMIDE

A process for the preparation of enzalutamide. The disclosed process may be effectively implemented on an industrial scale. In some implementations, the following reaction step is employed in the production of enzalutamide.

IMIDAZOLE DIKETONE COMPOUND AND USE THEREOF

Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.

A PROCESS FOR PRODUCING ENZALUTAMIDE

This invention provides a new process for producing enzalutamide of formula I, starting from the intermediate of formula XI, which cyclizes with the isothiocyanate of formula VIII in the presence of a base, an alcohol of the general formula R-OH as an additive, in a suitable solvent, wherein R is an alkyl with the number of carbon atoms C1C20, or a substituted alkyl with the number of carbon atoms C1C20, an aryl with the number of carbon atoms C6-C16, or a substituted aryl with the number of carbon atoms C6-C16.