633327-10-3

Usage

Uses

Used in Pharmaceutical Industry:
2,4-Difluoro-5-formylbenzonitrile is used as a synthetic intermediate for the development of various pharmaceuticals. Its unique structure allows it to be a key component in the creation of new drugs, contributing to the advancement of medicinal chemistry.
Used in Agrochemical Industry:
In the agrochemical sector, 2,4-Difluoro-5-formylbenzonitrile is utilized as a building block in the synthesis of agrochemicals. Its reactivity and structural features make it suitable for the production of compounds that can be used in crop protection and other agricultural applications.
Used in Organic Synthesis:
2,4-Difluoro-5-formylbenzonitrile is employed as a versatile reactant in organic synthesis. Its ability to participate in a range of chemical reactions enables the production of diverse compounds, making it a valuable asset for researchers and industries in the development of novel chemical entities.

Upstream product

• 452-76-6 2,4-difluorotoluene 
• 329314-68-3 2,4-difluoro-5-methylbenzonitrile 
• 333447-42-0 1,5-difluoro-2-iodo-4-methylbenzene 
• 473416-91-0 5-bromo-2,4-difluorobenzaldehyde 
• 544-92-3 copper(I) cyanide 

Relevant academic research and scientific papers

2. 4 - difluoro - 5 - (phthalazinone - 1 - methyl) - benzoyl piperazine compound and use thereof

The invention relates to a 2,4-difluoro-5-(phthalazone-1-methyl)-benzoyl piperazine compound and application of the 2,4-difluoro-5-(phthalazone-1-methyl)-benzoyl piperazine compound. Specifically, the invention discloses a compound of the structure shown in the formula I, wherein the definition of the compound of the structure shown in the formula I can be seen in the specification. The compound has the excellent PARP activity inhibitory effect and the excellent antitumor effect.

Discovery of potent 2,4-difluoro-linker poly(ADPribose) polymerase 1 inhibitors with enhanced water solubility and in vivo anticancer efficacy

Poly (ADP-ribose) polymerase 1 (PARP1) is overexpressed in a variety of cancers, especially in breast and ovarian cancers; tumor cells that are deficient in breast cancer gene 1/2 (BRCA1/2) are highly sensitive to PARP1 inhibition. In this study, we identified a series of 2,4-difluorophenyl-linker analogs (15-55) derived from olaparib as novel PARP1 inhibitors. Four potent analogs 17, 43, 47, and 50 (IC50=2.2-4.4 nmol/L) effectively inhibited the proliferation of Chinese hamster lung fibroblast V-C8 cells (IC50=3.2-37.6 nmol/L) in vitro, and showed specificity toward BRCA-deficient cells (SI=40-510). The corresponding hydrochloride salts 56 and 57 (based on 43 and 47) were highly water soluble in pH=1.0 buffered salt solutions (1628.2 μg/mL, 2652.5 μg/mL). In a BRCA1-mutated xenograft model, oral administration of compound 56 (30 m?kg-1d-1, for 21 d) exhibited more prominent tumor growth inhibition (96.6%) compared with the same dose of olaparib (56.3%); in a BRCA2-mutated xenograft model, oral administration of analog 43 (10 m?kg-1d-1, for 28 d) significantly inhibited tumor growth (69.0%) and had no negative effects on the body weights. Additionally, compound 56 exhibited good oral bioavailability (F=32.2%), similar to that of olaparib (F=45.4%). Furthermore, the free base 43 of the hydrochloride salt 56 exhibited minimal hERG inhibition activity (IC50=6.64 μmol/L). Collectively, these data demonstrate that compound 56 may be an excellent drug candidate for the treatment of cancer, particularly BRCA-deficient tumors.

PYRAZOLE COMPOUND AND MEDICINAL COMPOSITION CONTAINING THE SAME

The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 designates -(CO)h-(NRa)j-(CRb=CRc)k-Ar (wherein Ra, Rb and Rc each independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted C1-6 alkyl group or the like; Cy designates a 5- or 6-membered heteroaryl; and V each independently designate the formula -L-X-Y (wherein L designates a single bond, an optionally substituted C1-6 alkylene group or the like; X designates a single bond or the formula -A- (wherein A designates NR2, O, CO, S, SO or SO2) and so on; and Y designates a hydrogen atom, a halogen atom, nitro group or the like).