113237-20-0

Basic information

• Product Name: 2,6-DICHLORO-5-FLUORONICOTINAMIDE
• Synonyms: 2,6-DICHLORO-5-FLUOROPYRIDINE-3-CARBOXAMIDE;2,6-DICHLORO-5-FLUORONICOTINAMIDE;2,6-Dichloro-5-fluoronicotinamide 97%;2,6-Dichloro-5-fluoropyridine-3-carboxamide, 3-Carbamoyl-2,6-dichloro-5-fluoropyridine;3-PyridinecarboxaMide, 2,6-dichloro-5-fluoro-;2,6-Dichloro-5-fluoronicotinamide97%
• CAS NO: 113237-20-0
• Molecular Formula: C₆H₃Cl₂FN₂O
• Molecular Weight: 209.01
• Mol File: 113237-20-0.mol
• Article Data: 38

Chemical Properties

• Melting Point: 160-162
• Boiling Point: 259.0±40.0 °C(Predicted)
• Appearance: /
• Density: 1.614±0.06 g/cm3(Predicted)
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: 13.36±0.50(Predicted)
• CAS DataBase Reference: 2,6-DICHLORO-5-FLUORONICOTINAMIDE(CAS DataBase Reference)
• NIST Chemistry Reference: 2,6-DICHLORO-5-FLUORONICOTINAMIDE(113237-20-0)
• EPA Substance Registry System: 2,6-DICHLORO-5-FLUORONICOTINAMIDE(113237-20-0)

Safety Data

• Hazard Codes: Xi
• Hazardous Substances Data: 113237-20-0(Hazardous Substances Data)

Usage

General Description

2,6-Dichloro-5-fluoronicotinamide is a chemical compound with the molecular formula C6H3Cl2FN2O. It is a substituted nicotinamide derivative and a member of the pyridine family. 2,6-DICHLORO-5-FLUORONICOTINAMIDE is commonly used in the pharmaceutical industry as an intermediate for the synthesis of various pharmaceutical compounds, as well as in the field of agrochemicals for the production of crop protection products. It is also used as a reagent in organic synthesis and chemical research. 2,6-Dichloro-5-fluoronicotinamide is a white to off-white crystalline solid that is stable under standard conditions and can be stored at room temperature. It should be handled and stored according to good laboratory practices and local regulations.

Upstream product

• 75993-41-8 5-fluoro-2,6-dihydroxynicotinamide 
• 96568-02-4 2,6-dichloro-5-fluoro-3-nicotinoyl chloride 
• 82671-06-5 2,6-dichloro-5-fluoro-3-pyridinecarboxylic acid 
• 100-70-9 2-Cyanopyridine 
• 82671-02-1 2,6-dichloro-5-fluoro-pyridine-3-carbonitrile 
• 107-06-2 1,2-dichloro-ethane 

Downstream Products

• 82671-06-5 2,6-dichloro-5-fluoro-3-pyridinecarboxylic acid 
• 152840-65-8 2,6-dichloro-5-fluoropyridine-3-amine 
• 113237-22-2 ethyl 6-(4-acetyl-1-piperazinyl)-2-ethylamino-5-fluoronicotinate 
• 1312693-67-6 tert-butyl 4,6-dichloro-7-fluoro-3-oxo-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxylate 
• 1312693-69-8 4,6-dichloro-7-fluoro-1H-pyrrolo[3,4-c]pyridin-3(2H)-one 
• 75302-64-6 2-chloro-5-fluoropyridine-3-carboxamide 

Relevant articles and documents

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

KRASG12C has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to disrupt signaling by this long-"undruggable" target; however clinically viable inhibitors have yet to be identified. Here, we report efforts to exploit a cryptic pocket (H95/Y96/Q99) we identified in KRASG12C to identify inhibitors suitable for clinical development. Structure-based design efforts leading to the identification of a novel quinazolinone scaffold are described, along with optimization efforts that overcame a configurational stability issue arising from restricted rotation about an axially chiral biaryl bond. Biopharmaceutical optimization of the resulting leads culminated in the identification of AMG 510, a highly potent, selective, and well-tolerated KRASG12C inhibitor currently in phase I clinical trials (NCT03600883).

Pyridopyrimidinone compound and application thereof

The invention provides a pyridopyrimidinone compound with a structure as shown in a general formula (II) and application thereof. Researches prove that the compound provided by the invention can effectively inhibit KRAS G12C mutation. KRAS mutation accounts for a large proportion in tumors, no approved drug is obtained for treatment at present, and the compound provided by the invention has the potential to become a therapeutic drug for malignant tumors (especially non-small cell lung cancer (NSCLC) and colorectal cancer) carrying KRAS G12C mutation, and has a great application value.

IMPROVED SYNTHESIS OF KRAS G12C INHIBITOR COMPOUND

The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.