40352-92-9

Upstream product

• 113293-42-8 2-carboxy-5-chlorophenyl azide 
• 89-77-0 2-Amino-4-chlorobenzoic acid 

Downstream Products

• 328571-58-0 N-(2-azido-4-chlorobenzoyl)-δ-valerolactam 
• 113293-40-6 3,6-dichloro-2-(2,4-dichlorophenyl)-2 H-indazole 
• 113293-39-3 2-azido-4-chloro-N-(2,4-dichlorophenyl)benzamide 
• 1287677-38-6 C₁₉H₁₄ClN₅O 

Relevant academic research and scientific papers

Synthesis and SAR studies of novel benzodiazepinedione-based inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB)

Synthesis and structure-activity relationships (SAR) of a novel series of benzodiazepinedione-based inhibitors of Clostridium difficile toxin B (TcdB) are described. Compounds demonstrating low nanomolar affinity for TcdB, and which possess improved stability in mouse plasma vs. earlier compounds from this series, have been identified. Optimized compound 11d demonstrates a good pharmacokinetic (PK) profile in mouse and hamster and is efficacious in a hamster survival model of Clostridium difficile infection.

Synthesis of Diverse Nitrogen Heterocycles via Palladium-Catalyzed Tandem Azide–Isocyanide Cross-Coupling/Cyclization: Mechanistic Insight using Experimental and Theoretical Studies

A rapid and elegant tandem azide–isocyanide cross-coupling/cyclization protocol has been developed based on a nitrene transfer reaction. The palladium-catalyzed ligand-free methodology led to the synthesis of three different heterocyclic scaffolds with excellent atom/step/redox economy. Studies based on first-principles-based quantum calculations and control experiments unraveled a concerted process of nitrene transfer reaction on isocyanides, ruling out the metallaaziridine intermediate reported earlier. This finding could pave the way for novel applications of nitrene transfer reactions to generate bioactive heterocycles. (Figure presented.).

NOVEL CLOSTRIDIUM DIFFICILE TOXIN INHIBITORS

The present invention relates to benzodiazepine derivative compounds of formula (I), or pharmaceutically acceptable salts thereof. The present benzodiazepine compounds are useful Clostridium difficile inhibitors in the treatment of Clostridium difficile infection in humans. The present invention provides a pharmaceutical composition containing benzodiazepine compounds of formula (I) and a method of making as well as a method of using the same in treating patients infected with Clostridium difficile infection by administering the same. The compounds of the present invention may be used in combination with additional antibiotics or anti-toxin antibody drugs.

Total synthesis of rutaecarpine and analogues by tandem azido reductive cyclization assisted by microwave irradiation

The total synthesis of rutaecarpine and several analogues has been developed by using an azido reductive cyclization process starting from substituted azido benzoic acids. The intramolecular azido reductive cyclization step was performed with triphenylphosphine or Ni2B in HCl-MeOH (1 M) using microwave irradiation. This synthetic route is amenable for the generation of a library of quinazolinone compounds. Georg Thieme Verlag Stuttgart - New York.

Chemoenzymatic synthesis of pyrrolo[2,1-b]quinazolinones: Lipase-catalyzed resolution of vasicinone

A facile synthesis of bronchodilatory pyrrolo[2,1-b]quinazoline alkaloids by azidoreductive cyclization strategy employing TMSCl-NaI and bakers' yeast is described. Both the chemical and enzymatic methods are mild and take place at room temperature in good yields. Further, synthesis and resolution of vasicinone has been carried out by employing different lipases. It has been observed that lipase PS provides acetate of (S)-vasicinone in 98% ee.

Benzoheterocyclic fungicides

Compounds of any one of formulae I - VII where, ....is a single or double bond;, A is oxygen or sulphur;, R1 is aryl;, R2 is 1-imidazolyl or 1,2,4-triazol-1-yl; and, R3, R4, R5 and R6 which may be the same or different, ar