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Upstream product

• 98-03-3 thiophene-2-carbaldehyde 
• 136-95-8 2-amino-benzthiazole 
• 62-53-3 aniline 

Relevant academic research and scientific papers

Synthesis, spectral, antimicrobial and antitumor assessment of Schiff base derived from 2-aminobenzothiazole and its transition metal complexes

N-(thiophen-2-ylmethylene)benzo[d]thiazol-2-amine Schiff base (L) derived from 2-aminobenzothiazole and 2-thiophenecarboxaldehyde was synthesized and characterized using elemental analysis, IR, mass spectra, 1H NMR and UV-vis spectra. Its complexes with Cu(II), Fe(III), Ni(II) and Zn(II) were prepared and isolated as solid products and characterized by elemental and thermal analyses, spectral techniques as well as magnetic susceptibility. The IR spectra showed that the Schiff base under investigation behaves as bidentate ligand. The UV-vis spectra and magnetic moment data suggested octahedral geometry around Cu(II) and Fe(III) and tetrahedral geometry around Ni(II) and Zn(II). In view of the biological activity of the Schiff base and its complexes, it has been observed that the antimicrobial activity of the Schiff base increased on complexation with the metal ion. In vitro antitumor activity assayed against five human tumor cell lines furnished the significant toxicities of the Schiff base and its complexes.

Organocatalytic Asymmetric Synthesis of Benzothiazolopyrimidines via [4 + 2] Cyclization of 2-Benzothiazolimines and Aldehydes

We report the direct asymmetric synthesis of pyrimido[2,1-b]benzothiazoles using a commercially available chiral amine catalyst. A variety of 2-benzothiazolimines and aldehydes were well tolerated under the reaction conditions and generated the corresponding products in 81-99% yields with excellent diastereoselectivities and enantioselectivities (up to >20:1 dr, 99% ee). Furthermore, the products could be easily converted to other useful chiral building blocks.

Organocatalytic asymmetric [4+2] cyclization of 2-benzothiazolimines with azlactones: Access to chiral benzothiazolopyrimidine derivatives

An organocatalytic asymmetric domino Mannich/cyclization reaction between 2-benzothiazolimines with azlactones has been successfully developed. With the bifunctional squaramide catalyst, this formal [4+2] cyclization occurs with good to high yields and excellent stereoselectivities (up to 99% ee, >20?:?1 dr), providing an efficient and mild access to chiral benzothiazolopyrimidines bearing adjacent tertiary and quaternary stereogenic centers.

Benzothiazole analogues: Synthesis, characterization, MO calculations with PM6 and DFT, in silico studies and in vitro antimalarial as DHFR inhibitors and antimicrobial activities

Benzothiazole analogues are of interest due to their potential activity against malarial and microbial infections. In search of suitable antimicrobial and antimalarial agents, we report here the synthesis, characterization and biological activities of benzothiazole analogues (J 1-J 10). The molecules were characterized by IR, Mass, 1H NMR, 13C NMR and elemental analysis. The in vitro antimicrobial activity was investigated against pathogenic strains; the results were explained with the help of DFT and PM6 molecular orbital calculations. In vitro cytotoxicity and genotoxicity of the molecules were studied against S. pombe cells. In vitro antimalarial activity was studied. The active compounds J 1, J 2, J 3, J 5 and J 6 were further evaluated for enzyme inhibition efficacy against the receptor Pf-DHFR, computational and in vitro studies were carried out to examine their candidatures as lead dihydrofolate reductase inhibitors.

Access to Amide from Aldimine via Aerobic Oxidative Carbene Catalysis and LiCl as Cooperative Lewis Acid

Herein, an efficient route to amides from aldimines via aza-Breslow intermediates through aerobic oxidative carbene catalysis with LiCl as a cooperative Lewis acid is described. Many of the obtained N-heteroarylamides feature biological activity. Ambient

Synthesis of Some New Thienylazetidin-2-ones and Thienylthiazolidin-4-ones

A series of thienylidene anils (Ia, b-VIa, b) have been prepared by the interaction of thiophene-2-carboxaldehyde or its 5-bromo derivative with heterocyclic amines.Cyclocondensation reaction with chloroacetyl chloride or mercaptoacetic acid with thienyli