330792-69-3

Usage

Uses

Used in Chemical Synthesis:
Propanedinitrile, 2-[Methoxy(4-phenoxyphenyl)Methylene]is used as a key intermediate in the synthesis of a variety of organic compounds due to its reactive functional groups and structural properties.
Used in Laboratory Experiments:
As a chemical reagent, Propanedinitrile, 2-[Methoxy(4-phenoxyphenyl)Methylene]is employed in laboratory experiments for its ability to facilitate specific chemical reactions and to study its properties and behavior under controlled conditions.
Used in Dye Production:
Propanedinitrile, 2-[Methoxy(4-phenoxyphenyl)Methylene]is used as a precursor in the production of dyes, contributing to the development of colorants for various applications, including textiles, plastics, and printing inks.
Used in Pharmaceutical Industry:
In the pharmaceutical sector, Propanedinitrile, 2-[Methoxy(4-phenoxyphenyl)Methylene]is utilized in the development of new drugs, potentially serving as an active pharmaceutical ingredient or a crucial component in the synthesis of medicinal compounds.
Used in Agrochemicals:
Propanedinitrile, 2-[Methoxy(4-phenoxyphenyl)Methylene]is also used in the agrochemical industry, where it may be involved in the creation of pesticides, herbicides, or other agricultural chemicals to enhance crop protection and yield.
Used in Medicine and Biotechnology:
Due to its biological activities, Propanedinitrile, 2-[Methoxy(4-phenoxyphenyl)Methylene]is explored for potential applications in medicine and biotechnology, possibly serving as a therapeutic agent or a tool in biotechnological processes.

Upstream product

• 18107-18-1 diazomethyl-trimethyl-silane 
• 330792-68-2 2-[hydroxy-(4-phenoxy-phenyl)-methylene]-malononitrile 
• 77-78-1 dimethyl sulfate 
• 67-56-1 methanol 
• 149-73-5 trimethyl orthoformate 
• 1623-95-6 4-phenoxybenzoyl chloride 
• 109-77-3 malononitrile 
• 459-57-4 4-fluorobenzaldehyde 
• 108-95-2 phenol 
• 619-44-3 methyl 4-iodobenzoate 
• 21218-94-0 methyl 4-phenoxybenzoate 
• 2215-77-2 4-Phenoxybenzoic acid 

Downstream Products

• 1207476-93-4 C₂₄H₁₉N₃O₂ 
• 1418272-57-7 C₃₃H₃₉N₇O₅ 
• 1418270-10-6 (R,E)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-4-(2-methoxyethylamino)but-2-en-1-one 
• 1418272-59-9 C₂₅H₂₃BrN₆O₂ 
• 1418272-63-5 C₃₃H₃₇N₇O₄ 
• 1418270-73-1 (R,E)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-4-(cyclopropylamino)but-2-en-1-one 
• 1418270-14-0 (R,E)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-4-((2-methoxyethyl)(methyl)amino)but-2-en-1-one 
• 1418272-69-1 C₂₃H₁₆N₆O₃ 
• 1418272-70-4 C₂₈H₂₄N₆O₅ 
• 1418272-71-5 C₂₈H₂₆N₆O₃ 
• 1418272-72-6 C₂₉H₂₈N₆O₃ 
• 1418270-24-2 (R,E)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-4-(methyl(pyridin-2-yl)amino)but-2-en-1-one 
• 1418270-28-6 (R,E)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-4-(dicyclopropylamino)but-2-en-1-one 
• 330786-24-8 3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 

Relevant academic research and scientific papers

PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR

Disclosed is a process for the preparation of certain intermediates, e.g. process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof, in an enantioenriched form, which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.

Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor

Therapeutic combinations of a proteasome inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of a proteasome inhibitor and a BTK inhibitor and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.

Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

Potent covalent inhibitors of Bruton's tyrosine kinase (BTK) based on an aminopyrazole carboxamide scaffold have been identified. Compared to acrylamide-based covalent reactive groups leading to irreversible protein adducts, cyanamide-based reversible-covalent inhibitors provided the highest combined BTK potency and EGFR selectivity. The cyanamide covalent mechanism with BTK was confirmed through enzyme kinetic, NMR, MS, and X-ray crystallographic studies. The lead cyanamide-based inhibitors demonstrated excellent kinome selectivity and rat pharmacokinetic properties.

TREATMENT OF INDOLENT OR AGGRESSIVE B-CELL LYMPHOMAS USING A COMBINATION COMPRISING BTK INHIBITORS

Disclosed herein is a method for the prevention, delay of progression or treatment of indolent or aggressive B-cell lymphomas in an individual in need thereof, comprising administering a Btk inhibitor (in particularly (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo-[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof) in combination with an anti-PD-1 antibody. The potent and selective BTK inhibitor in combination with the anti-PD-1 antibody have a manageable toxicity profile in patients with indolent and aggressive lymphomas.

Catalytic Azido-Hydrazination of Alkenes Enabled by Visible Light: Mechanistic Studies and Synthetic Applications

A visible-light-enabled catalytic intermolecular azido-hydrazination method for unactivated alkenes is developed via an orderly radical addition sequence. This transformation features metal-free and redox-neutral conditions and is applicable to a wide range of alkenes with commercially available reagents. Mechanistic and kinetic studies reveal that the efficient generation of azide radical enabled by fluorenone under visible-light is critical to this methodology. The β-azido alkyl hydrazines prepared with this reaction can be conveniently derived to valuable synthetic building blocks, and one of the products has been successfully applied in the total synthesis of (±)-ibrutinib, which is used to treat B cell cancers. (Figure presented.).

Method for preparing ibrutinib

The invention discloses a method for preparing ibrutinib. The method includes the following steps of 1, preparation of IB-A, 2, preparation of IB-B, 3, preparation of IB-C, 4, preparation of IB-D, 5,preparation of IB-E, 6, preparation of IB-F, 7, preparation of IB-G, 8, preparation of IB-H, and 9, preparation of IB-J. The method has the advantages that the process is mature and stable, the quality of the product is stable, the production process is safe and reliable, and the ibrutinib is suitable for industrial production.

USE OF A COMBINATION COMPRISING A BTK INHIBITOR FOR TREATING CANCERS

A method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a targeted therapy agent. A pharmaceutical combination comprising a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a targeted therapy agent.

CRYSTALLINE FORM OF (S)-7-(1-ACRYLOYLPIPERIDIN-4-YL)-2-(4-PHENOXYPHENYL)-4,5,6,7-TETRAHYDROPYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF

The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.

CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF

The present invention relates to a crystalline form of (S) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahydropyrazolo [1, 5-a] pyri midine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.

Methods of Using BTK Inhibitors to Treat Dermatoses

In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat dermatoses, such as psoriasis, atopic dermatitis, contact dermatitis, scleroderma, and cutaneous lupus erythematosus. In other embodiments, the methods of the invention further comprise the step of administering a therapeutically effective dose of an anti-inflammatory agent.