1021298-68-9

Usage

Uses

Used in Pharmaceutical Industry:
2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)Methyl)benzonitrile is used as an intermediate in the synthesis of phthalazinone scaffolds, which are potent inhibitors of poly(ADP-ribose) polymerase. These scaffolds have potential applications in the development of therapeutic agents for various diseases, including cancer and neurodegenerative disorders, due to their ability to modulate cellular processes and pathways.

Upstream product

• 763114-25-6 2-fluoro-5-(3-oxo-1,3-dihydroisobenzofuranylidene methyl)benzonitrile 
• 77771-02-9 3-bromo-4-fluorobenzaldehyde 
• 218301-22-5 2-fluoro-5-formylbenzonitrile 
• 119-67-5 o-carboxybenzaldehyde 
• 61260-15-9 dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphonate 

Downstream Products

• 763114-26-7 2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid 
• 1379676-65-9 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1 -yl)methyl)benzoyl)-1 ,4-diazepan-1-yl)-3,3-dimethylbutane-1,2-dione 
• 763114-04-1 tert-butyl 4-[2’-fluoro-5’-[(4’’-oxo-3’’H-phthalazin-1’’-yl)methyl]benzoyl]piperazine-1-carboxylate 
• 1379676-53-5 1-cyclopropyl-2-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)ethane-1,2-dione 
• 874116-49-1 tert-butyl 4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)-1,4-diazepane-1-carboxylate 
• 1379676-60-4 1-cyclopropyl-2-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)-1,4-diazepan-1-yl) ethane-1,2-dione 
• 1379676-62-6 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-2-phenylethane-1,2-dione 
• 1379676-64-8 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-3,3-dimethylbutane-1,2-dione 
• 1379676-66-0 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)-1,4-diazepan-1-yl)-2-phenylethane-1,2-dione 
• 1379676-67-1 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)-1,4-diazepan-1-yl)-2-(furan-2-yl)ethane-1,2-dione 
• 1379676-69-3 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-2-(furan-2-yl)ethane-1,2-dione 
• 1379676-73-9 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)propane-1,2-dione 
• 1379676-75-1 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)-1,4-diazepan-1-yl)propane-1,2-dione 
• 763113-22-0 olaparib 

Relevant academic research and scientific papers

Synthesis, Cytotoxicity, and Mechanistic Investigation of Platinum(IV) Anticancer Complexes Conjugated with Poly(ADP-ribose) Polymerase Inhibitors

Many clinical trials using combinations of platinum drugs and PARP-1 inhibitors (PARPi) have been carried out, with the hope that such combinations will lead to enhanced therapeutic outcomes against tumors. Herein, we obtained seven potential PARPi with structural diversity and then conjugated them with cisplatin-based platinum(IV) complexes. Both the synthesized PARPi ligands and PARPi-Pt conjugates [PARPi-Pt(IV)] show inhibitory effects against PARP-1's catalytic activity. The PARPi-Pt(IV) conjugates are cytotoxic in a panel of human cancer cell lines, and the leading ones display the ability to overcome cisplatin resistance. A mechanistic investigation reveals that the representative PARPi-Pt(IV) conjugates efficiently enter cells, bind to genomic DNA, disturb cell cycle distribution, and induce apoptotic cell death in both cisplatin-sensitive and-resistant cells. Our study provides a strategy to improve the cytotoxicity of platinum(IV)-based anticancer complexes and overcome cisplatin resistance by using a small-molecule anticancer complex that simultaneously damages DNA and inhibits PARP.

Preparation method of Olaparib

The invention discloses a preparation method of Olaparib. The preparation method of the Olaparib comprises the steps that: Compound III is prepared by an amidation reaction of compound II under a condition of AlMe3, and the compound III is hydrolyzed to react with methanone,cyclopropyl-1-piperazinyl to obtain a final quality product of olaparib (I) by refining. The preparation method has a simpleroute, is easy to operate, has a high total product yield, has few byproducts, and is suitable for industrial production.

HETEROCYCLIC DERIVATES, PREPARATION PROCESSES AND MEDICAL USES THEREOF

Disclosed are heterocyclic derivatives, methods for making them, compositions containing the same and uses thereof. Particularly, their pharmaceutical use as inhibitors of PARP is disclosed.

PHTHALAZINONE DERIVATIVE

4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.