654073-32-2

Usage

Uses

Used in Pharmaceutical Industry:
1-Azetidinesulfonamide(9CI) is used as an antimicrobial agent for its inherent antibiotic and antifungal properties, contributing to the development of treatments for a range of infections caused by susceptible microorganisms.
Used in Medicinal Chemistry Research:
1-Azetidinesulfonamide(9CI) is utilized as a key intermediate in the synthesis of various organic compounds, facilitating the advancement of new drug discovery and the enhancement of existing pharmaceutical formulations.
Used in Organic Synthesis:
1-Azetidinesulfonamide(9CI) is employed as a building block in organic synthesis, enabling the creation of novel compounds with potential applications in various chemical and material science fields.

Upstream product

• 503-29-7 azetidine 
• 96042-30-7 4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran 
• 1271835-78-9 benzyl (azetidin-1-ylsulfonyl)carbamate 

Downstream Products

• 1204707-71-0 N-[2-[(2,3-difluorophenyl)methylsulfanyl]-6-[[(1R,2R)-2,3-dihydroxy-1-methyl-propyl]amino]pyrimidin-4-yl]azetidine-1-sulfonamide 
• 1204707-81-2 N-[2-[(2,3-difluorobenzyl)thio]-6-({(1R)-1-[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]ethyl}amino)pyrimidin-4-yl]azetidine-1-sulfonamide 
• 1204707-83-4 N-[2-[(2,3-difluorobenzyl)thio]-6-({(1R)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethyl}amino)pyrimidin-4-yl]azetidine-1-sulfonamide 
• 1204707-87-8 (N-[2-[(2,3-difluorobenzyl)thio]-6-({(1S)-1-[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]ethyl}amino)pyrimidin-4-yl]azetidine-1-sulfonamide) 
• 1204707-89-0 N-[2-[(2,3-difluorobenzyl)thio]-6-({(1S)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethyl}amino)pyrimidin-4-yl]azetidine-1-sulfonamide 
• 1443431-33-1 N-(azetidin-1-ylsulfonyl)-5-chloro-4-{[(5-chloro-6-cyclopropylpyridin-3-yl)oxy]methyl}-2-fluorobenzamide 
• 1443431-23-9 N-(azetidin-1-ylsulfonyl)-4-{[(5-chloro-6-isopropoxypyridin-3-yl)oxy]methyl}-2,5-difluorobenzamide 
• 1446444-51-4 N-(azetidin-1-ylsulfonyl)-5-chloro-4-{[5-chloro-6-(2,2,3,3-tetrafluoropropoxy)pyridin-3-yl]oxy}-2-fluorobenzamide 
• 1446444-52-5 N-(azetidin-1-ylsulfonyl)-5-chloro-4-(3,4-dichlorophenoxy)-2-fluorobenzamide 

Relevant academic research and scientific papers

7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones designed by a “cut and glue” strategy are dual aurora a/vegf-r kinase inhibitors

Although overexpression and hyperactivity of protein kinases are causative for a wide range of human cancers, protein kinase inhibitors currently approved as cancer drugs address only a limited number of these enzymes. To identify new chemotypes addressing alternative protein kinases, the basic structure of a known PLK1/VEGF-R2 inhibitor class was formally dissected and reassembled. The resulting 7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones were synthesized and proved to be dual inhibitors of Aurora A kinase and VEGF receptor kinases. Crystal structures of two representatives of the new chemotype in complex with Aurora A showed the ligand orientation in the ATP binding pocket and provided the basis for rational structural modifications. Congeners with attached sulfamide substituents retained Aurora A inhibitory activity. In vitro screening of two members of the new kinase inhibitor family against the cancer cell line panel of the National Cancer Institute (NCI) showed antiproliferative activity in the single-digit micromolar concentration range in the majority of the cell lines.

Improved Synthesis of the Nav1.7 Inhibitor GDC-0276 via a Highly Regioselective SNAr Reaction

The development of a redesigned and improved second-generation synthesis of the Nav1.7 inhibitor GDC-0276 based on experience gained from a fit-for-purpose first-generation synthesis will be described. The first-generation synthesis proceeded via a regioselective SNAr reaction on the advanced starting material t-butyl 5-chloro-2,4-difluorobenzoate with 1-adamantanemethanol. In the newly developed second-generation synthesis, the much improved regioselective SNAr reaction was performed on the readily available starting material 1-chloro-2,4-difluorobenzene, followed by installation of the carboxylate group by electrophilic aromatic bromination and a palladium-catalyzed alkoxycarbonylation. A subsequent Suzuki-Miyaura cross-coupling reaction was then telescoped directly into a phase-transfer-catalyzed ester hydrolysis. Amidation of the resulting acid intermediate with 1-azetidine sulfamide in turn provided GDC-0276 in high overall yield and purity on a 100 kg scale.

SULFONAMIDE DERIVATIVES

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav 1

N-AMINOSULFONYL BENZAMIDES

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulphonamide Nav 1.7 inhibitors of formula (I) or a pharmaceutically acceptable salt thereof, wherein Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description. Nay 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain

Macrocyclic compounds as inhibitors of viral replication

The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

PYRIMIDYL SULPHONE AMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid