1235865-75-4

Basic information

• Product Name: abt199 int 2
• Synonyms: abt199 int 2;methyl 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-fluorobenzoate;ABT199 intermediate 3;ABT199 intermediates;Methyl 2-((1H-pyrrolo[2,3-b]pyrin- 5-yl)oxy)-4-fluorobenzoate;ABT-199 Intermediate;methyl 4-fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate;Methyl-2-((1H-pyrrolo[2,3-b]pyridine-5-yl)oxy)-4-fluorobenzoate
• CAS NO: 1235865-75-4
• Molecular Formula: C₁₅H₁₁FN₂O₃
• Molecular Weight: 286.2578432
• EINECS: -0
• Mol File: 1235865-75-4.mol
• Article Data: 18

Chemical Properties

• Appearance: /
• Density: 1.377±0.06 g/cm3(Predicted)
• Storage Temp.: Sealed in dry,Room Temperature
• PKA: 13.21±0.40(Predicted)
• CAS DataBase Reference: abt199 int 2(CAS DataBase Reference)
• NIST Chemistry Reference: abt199 int 2(1235865-75-4)
• EPA Substance Registry System: abt199 int 2(1235865-75-4)

Safety Data

• Hazardous Substances Data: 1235865-75-4(Hazardous Substances Data)

Usage

Uses

Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate is the intermediate for ABT 199 (A112430), which is a potent and selective BCL-2 inhibitor that achieves potent antitumor activity while sparing platelets. It’s practical application is to treat chronic lymphocytic leukaemic cells and estrogen receptor-positive breast cancer.

Upstream product

• 1583-58-0 2,4-difluoro-benzoic acid 
• 67-56-1 methanol 
• 98549-88-3 5-hydroxypyrrolo[2,3-b]pyridine 
• 106614-28-2 methyl 2,4-difluorobenzoate 
• 858116-66-2 5-bromo-1-(triisopropylsilyl)-1H-pyrrolo[2,3-b]pyridine 
• 685514-01-6 1-[tris(propan-2-yl)silyl]-1H-pyrrolo[2,3-b]pyridin-5-ol 

Downstream Products

• 1235865-77-6 [2-((1H-pyrrolo [2,3-b]pyridin-5-yl)oxy)-4-(4-((4’-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1’-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid] 
• 1257044-40-8 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)phenyl)sulfonyl)benzamide 
• 1235865-76-5 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4’-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1’-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid methyl ester 

Relevant articles and documents

Heterocyclic compounds as BCL-2 inhibitor

The present invention relates to a compound, a pharmaceutical composition containing the same, preparation method of the compound and thepharmaceutical composition, and uses ofthe compound and the pharmaceutical compositionas B-cell lymphoma-2 (BCL-2) inhibitors, wherein the compound is a compound shown as a formula I, or an isomer, a prodrug, a solvate, a stable isotope derivative or a pharmaceutically acceptable salt thereof. The invention also relates to the uses of the compound or the composition containing the same in treatment or prophylaxis of BCL2-mediated related diseases such as tumours.

Solid dispersions containing an apoptosis-inducing agent

A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

PROCESS FOR THE PREPARATION OF VENETOCLAX

The present disclosure provides novel synthetic process for the preparation of venetoclax. The disclosed processes involve the use of novel intermediates. Processes for the preparation of these intermediates are also disclosed as well as methods for the preparation of particularly useful salts thereof.