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

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

• 74-89-5 methylamine 
• 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 
• 915087-24-0 2-fluoro-N-methyl-4-nitro-benzamide 
• 948717-18-8 2,4-difluoro-N-methylbenzamide 
• 72482-64-5 2,4-difluorobenzoyl 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 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.

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.

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.

Substituted diazaspiroalkanes as androgen receptor modulators

This invention provides for compounds of the Formula II: wherein A, B, Het, R1, R2 and R3 are as described herein. These compounds are androgen receptor modulators useful for the treatment of androgen receptor-associated conditions.

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.

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.