1034975-40-0

Usage

Uses

Used in Pharmaceutical Industry:
4-(4-methylpiperazin-1-yl)-2-[(tetrahydropyran-4-yl)amino]benzoic acid tert-butyl ester is used as a potential drug candidate for central nervous system disorders due to the presence of the piperazine moiety, which is commonly found in medications with such applications.
Used in Drug Formulation:
In the pharmaceutical industry, 4-(4-methylpiperazin-1-yl)-2-[(tetrahydropyran-4-yl)amino]benzoic acid tert-butyl ester is used to improve the stability and lipophilicity of drug formulations, thanks to its tert-butyl ester group, which may facilitate better absorption and bioavailability when administered orally.
Further research is necessary to explore the full range of properties and potential applications of 4-(4-methylpiperazin-1-yl)-2-[(tetrahydropyran-4-yl)amino]benzoic acid tert-butyl ester, including its pharmacological activity, safety profile, and optimal methods of synthesis and delivery.

Upstream product

• 29943-42-8 Tetrahydro-4H-pyran-4-one 
• 1034975-35-3 tert‐butyl 2‐amino‐4‐(4‐methylpiperazin‐1‐yl)benzoate 
• 942271-61-6 tert-butyl 4-(4-methylpiperazin-1-yl)-2-nitrobenzoate 
• 108-97-4 4-pyrone 
• 109-01-3 1-methyl-piperazine 
• 889858-12-2 4-bromo-2-fluoro-benzoic acid tert-butyl ester 
• 38041-19-9 4-aminotetrahydropyran 

Downstream Products

• 1034975-53-5 tert-butyl 4-(4-methylpiperazine-1-yl)-2-(2,2,2-trifluoro-N-(tetrahydro-2H-pyran-4-yl)acetamido)benzoate 
• 1034975-62-6 4-(4-methylpiperazine-1-yl)-2-(2,2,2-trifluoro-N-(tetrahydro-2H-pyran-4-yl)acetamido)benzoic acid trifluoroacetic acid salt 
• 1108743-60-7 N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide 
• 1108745-38-5 N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(2,2,2-trifluoro-N-(tetrahydro-2H-pyran-4-yl)acetamido)benzamide 
• 1034976-52-7 4-(4-methylpiperazin-1-yl)-2-[(tetrahydropyran-4-yl)-(2,2,2-trifluoroacetyl)amino]benzoyl chloride 

Relevant academic research and scientific papers

Total Synthesis of Entrectinib with Key Photo-Redox Mediated Cross-Coupling in Flow

By using photo-redox catalysis in flow the newly marketed drug entrectinib (referred to by the brand name Rozlytrek) was synthesized in 6 linear steps from readily available building blocks under mild conditions. Evaluation of multiple intermediates for their use in the critical C?N amination step in flow led to the finding that more electron deficient aryl-halides achieve higher conversion to the desired product. Data supports that more electron rich aryl-halides undergo a significant amount of hydro-dehalogenation compared to the productive C?N bond formation. Through evaluating various entry points into the synthesis of entrectinib, shorter routes were identified albeit in low yields. The modularity of this route will allow chemists to rapidly synthesize a diverse library of compounds through this route. Via different synthetic intermediates, a scale-up route was discovered for the synthesis of entrectinib using photo-redox in flow in less steps than previously reported, highlighting the utility of flow chemistry in the pharmaceutical industry.

Indazole compound for inhibiting kinase activity as well as composition and application thereof

The invention relates to an indazole compound for inhibiting kinase activity and relates to preparation and application of the indazole compound. Specifically, the invention discloses the indazole compound shown as a formula (I), or crystal forms, prodrugs, pharmaceutically acceptable salts, stereoisomers, tautomers, solvates or pharmaceutical compositions of hydrates of the indazole compound. Thecompound and the composition containing the compound, provided by the invention, have excellent inhibition performance on kinase protein, and also have better pharmacokinetics parameter characteristics at the same time; the medicine concentration of the compound in animals can be improved and the curative effect and safety of the medicine are improved. The formula (I) is shown in the description.

HETEROCYCLIC DERIVATIVES MODULATING ACTIVITY OF CERTAIN PROTEIN KINASES

The present invention relates to novel heterocyclic derivatives having general formula (I) and their therapeutic use for diseases such as cancer, inflammation, pain, autoimmune diseases or neurodegenerative diseases like Alzheimer's or Parkinson's disease that can be treated by modulation of certain protein kinases. Compounds of formula (I) can be used for treatment of patients who do not respond to kinase inhibition therapy that comprises currently available medications.

SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS

Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may

SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS

Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.