Polysubstituted pyrazoles, part 5. Synthesis of new 1-(4-chlorophenyl)-4-hydroxy-1H-pyrazole-3-carboxylic acid hydrazide analogs and some derived ring systems. A novel class of potential antitumor and anti-HCV agents.

We have developed a new method for C–H amination of aromatic compounds based on electrochemical oxidation of aromatic compounds in the presence of pyridine followed by the reaction of the resulting N-arylpyridinium ions with an alkylamine. This new transformation serves as a powerful method for synthesizing aromatic primary amines from aromatic compounds without using metal catalysts and harsh chemical reagents. High chemoselectivity of the present method is demonstrated by C–H amination of aromatic compounds bearing a nitro group to give a key intermediate for the synthesis of VLA-4 antagonist.

Electrochemical C-H amination: synthesis of aromatic primary amines via N-arylpyridinium ions.

Nitrogen‐, and/or Sulfur-Containing Heterocyclic Rings Poulomi Majumdar,†,‡ Anita Pati,†,§ Manabendra Patra, Rajani Kanta Behera,† and Ajaya Kumar Behera*,† †Organic Synthesis Laboratory, School of Chemistry, Sambalpur University, Jyoti Vihar, Burla 768019, Orissa, India ‡State Key Laboratory of Fine Chemicals, School of Chemical Engineering, Dalian University of Technology, Dalian, 116024, P.R. China School of Applied Sciences (Chemistry), KIIT University, Bhubaneswar 751024, India National Institute of Science & Technology, Palur Hill, Berhampur 761068, Orissa, India

Acid hydrazides, potent reagents for synthesis of oxygen-, nitrogen-, and/or sulfur-containing heterocyclic rings.

High Affinity Recognition of Serotonin Transporter Antagonists Defined by Species-scanning Mutagenesis AN AROMATIC RESIDUE IN TRANSMEMBRANE DOMAIN I DICTATES SPECIES-SELECTIVE RECOGNITION OF CITALOPRAM AND MAZINDOL

Protection for the Amino Group

A series of diarylsemicarbazones was synthesized and tested against human neoplastic cell lines. The more active members have a 1-naphthyl ring at the carbamidic nitrogen, and chloro, dimethylamino or nitro group substituents at the benzylidene moiety. None of these showed affinity to DNA. One of the more active compounds was tested as a topoisomerase I inhibitor and showed a potent effect. SAR studies demonstrated linear correlation between lypophilicity and activity on the most sensitive lines and a definite conformational shape for antineoplastic action.

Carlos H. Gaozza

Papers

Diarylsemicarbazones: synthesis, antineoplastic activity and topoisomerase I inhibition assay.

Kinetic study on the anelation of heterocycles. 2. pyrido[2,3-b]pyrazine and pyrido[3,4-b]pyrazine derivatives synthesized by the hinsberg reaction

Synthesis of pyridinium heterocyclic ylides. Degradation of the pyridinium group

Heterocycles derived from the condensation of aliphatic diamines with succinic and glutaric acid derivatives

Heterocycles derived from the condensation of 1,3‐propanediamine with phthalic acid derivatives