1237535-78-2

Basic information

• Product Name: 5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE
• Synonyms: 5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE;5-fluoro-1,2,3,4-tetrahydro-1,8-naphthyridin-2-one;EOS-60485;5-fluoro-3,4-dihydro-1,8-naphthyridin-2(1H)-one(WXFC0576)
• CAS NO: 1237535-78-2
• Molecular Formula: C₈H₇FN₂O
• Molecular Weight: 166.1523832
• Mol File: 1237535-78-2.mol
• Article Data: 10

Chemical Properties

• Boiling Point: 241.8±50.0 °C(Predicted)
• Appearance: /
• Density: 1.45±0.1 g/cm3(Predicted)
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: 1.90±0.20(Predicted)
• CAS DataBase Reference: 5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE(CAS DataBase Reference)
• NIST Chemistry Reference: 5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE(1237535-78-2)
• EPA Substance Registry System: 5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE(1237535-78-2)

Safety Data

• Hazardous Substances Data: 1237535-78-2(Hazardous Substances Data)

Usage

General Description

5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE is a chemical compound with the molecular formula C11H8FN3O. It is a derivative of 1,8-naphthyridine and its structure consists of a naphthyridine ring with a fluorine atom at the 5-position and a carbonyl group at the 2-position. 5-FLUORO-3,4-DIHYDRO-1,8-NAPHTHYRIDIN-2(1H)-ONE is known for its potential biological activity, particularly for its use as an anti-cancer agent, as it has been studied for its cytotoxic effects on cancer cells. Research has also shown that it can inhibit the formation of microtubules, which are involved in cell division, making it a potential candidate for anti-cancer drug development. Additionally, it has been investigated for its antibacterial and antifungal properties, showing promise as a potential therapeutic agent in the treatment of infectious diseases.

Upstream product

• 1237535-77-1 tert-butyl (4-fluoro-3-iodopyridin-2-yl)carbamate 
• 6044-68-4 3,3-dimethoxyprop-1-ene 
• 944401-77-8 4-fluoropyridin-2-amine 
• 34941-91-8 2-chloro-4-fluoropyridine 
• 1237535-76-0 4-fluoropyridin-2-ylcarbamic acid tert-butyl ester 
• 3054-95-3 acrylaldehyde diethyl acetal 

Downstream Products

• 1446090-79-4 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one 
• 1446090-78-3 5-(((1S,1aR,6bS)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropane[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one 

Relevant articles and documents

CHIRAL SYNTHESIS OF FUSED BICYCLIC RAF INHIBITORS

The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitor enantiomers of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, with high enantiomeric excess (%ee). The disclosure also relates to method of using the compound of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.

STABLE SOLID DISPERSIONS OF B-RAF KINASE DIMER INHIBITOR, METHODS OF PREPARATION, AND USES THEREFOR

Disclosed herein is a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1- ( (1S, 1aS, 6bS) -5- ( (7-oxo-5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-4-yl) oxy) -1a,6b-dihydro-1H-cyclopropa [b] benzofuran-1-yl) -3- (2, 4, 5-trifluorophenyl) urea and a specific stabilizing polymer, the method for preparing the same, and the uses of the solid dispersion. Also disclosed herein is the crystalline form of Compound 1.

Stable crystalline form A of B-RAF kinase dimer inhibitor

The invention relates to a stable crystalline form A of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl[b] benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1), a preparation method of the crystalline Form A and therapeutic use of the crystalline Form A.