Literature DB >> 33936753

Reduced 3,4'-bi-pyrazoles carrying thio-phene and thia-zole substituents: structures of two intermediates and two products.

Chayanna Harish Chinthal1, Hemmige S Yathirajan1, Nagaraja Manju2, Balakrishna Kalluraya2, Sabine Foro3, Christopher Glidewell4.   

Abstract

Cyclo-addition reactions between 3-(5-ar-yloxy-3-methyl-1-phenyl-1H-pyrazol-4-yl)-1-(thio-phen-2-yl)prop-2-en-1-ones and thio-semicarbazide leads to the formation of reduced 3,4'-bi-pyrazole-2-carbo-thio-amides. Further cyclo-addition of these inter-mediates with either diethyl acetyl-enedi-carboxyl-ate or 4-bromo-phenacyl bromide leads to reduced 3,4'-bi-pyrazoles carrying oxo-thia-zole or thia-zole substituents, respectively. The structures of two representative inter-mediates and two representative products established unambiguously the regiochemistry of the cyclo-addition reactions. The mol-ecules of 3'-methyl-5'-(2-methyl-phen-oxy)-1'-phenyl-5-(thio-phen-2-yl)-3,4-di-hydro-1'H,2H-3,4'-bi-pyra-zole-2-carbo-thio-amide, C25H23N5OS2 (Ia), are linked by N-H⋯N hydrogen bonds to form simple C(8) chains. The analogous compound 5'-(2,4-di-chloro-phen-oxy)-3'-methyl-1'-phenyl-5-(thio-phen-2-yl)-3,4-di-hydro-1'H,2H-3,4'-bi-pyra-zole-2-carbo-thio-amide hemihydrate crystallizes as a hemihydrate, C24H19Cl2N5OS2·0.5H2O (Ib), and the independent components are linked into a chain of spiro-fused R 4 4(20) rings by a combination of O-H⋯N and N-H⋯O hydrogen bonds. In the structure of ethyl (Z)-2-{2-[3'-methyl-1'-phenyl-5-(thio-phen-2-yl)-5'-(2-methyl-phen-oxy)-3,4-di-hydro-1'H,2H-3,4'-bi-pyrazole-2-yl]-4-oxo-4,5-di-hydro-thia-zol-5-yl-idene}acetate, C31H27N5O4S2 (II), inversion-related pairs of mol-ecules are linked by paired C-H⋯π(arene) hydrogen bonds to form cyclic centrosymmetric dimers, but there are no direction-specific inter-molecular inter-actions in 4-(4-bromo-phen-yl)-2-[5'-(2,4-di-chloro-phen-oxy)-3'-methyl-1'-phenyl-5-(thio-phen-2-yl)-3,4-di-hydro-1'H,2H-3,4'-bi-pyrazole-2-yl]-4-thia-zole, C32H22BrCl2N5OS2 (III). Comparisons are made with the structures of some related compounds. © Harish Chinthal et al. 2021.

Entities:  

Keywords:  crystal structure; heterocyclic compounds; hydrogen bonding; reduced bi­pyrazoles; regiochemistry; supra­molecular assembly; synthesis

Year:  2021        PMID: 33936753      PMCID: PMC8025870          DOI: 10.1107/S2056989021002310

Source DB:  PubMed          Journal:  Acta Crystallogr E Crystallogr Commun


  16 in total

1.  Regioselective reaction: synthesis, characterization and pharmacological studies of some new Mannich bases derived from 1,2,4-triazoles.

Authors:  Arun M Isloor; Balakrishna Kalluraya; Prashanth Shetty
Journal:  Eur J Med Chem       Date:  2009-05-05       Impact factor: 6.514

2.  PLATON SQUEEZE: a tool for the calculation of the disordered solvent contribution to the calculated structure factors.

Authors:  Anthony L Spek
Journal:  Acta Crystallogr C Struct Chem       Date:  2015-01-01       Impact factor: 1.172

3.  Conversion of substituted 5-aryloxypyrazolecarbaldehydes into reduced 3,4'-bipyrazoles: synthesis and characterization, and the structures of four precursors and two products, and their supramolecular assembly in zero, one and two dimensions.

Authors:  Haruvegowda Kiran Kumar; Hemmige S Yathirajan; Nagaraj Manju; Balakrishna Kalluraya; Ravindranath S Rathore; Christopher Glidewell
Journal:  Acta Crystallogr C Struct Chem       Date:  2019-05-23       Impact factor: 1.172

4.  Thiophene and benzodioxole appended thiazolyl-pyrazoline compounds: Microwave assisted synthesis, antimicrobial and molecular docking studies.

Authors:  S Shahavar Sulthana; S Arul Antony; C Balachandran; S Syed Shafi
Journal:  Bioorg Med Chem Lett       Date:  2015-05-22       Impact factor: 2.823

5.  Synthesis and pharmacological study of 1-acetyl/propyl-3-aryl-5-(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)-2-pyrazoline.

Authors:  K S Girisha; Balakrishna Kalluraya; Vijaya Narayana
Journal:  Eur J Med Chem       Date:  2010-07-24       Impact factor: 6.514

6.  Synthesis and antimicrobial activity of some new thiazole, thiophene and pyrazole derivatives containing benzothiazole moiety.

Authors:  Samir Bondock; Walid Fadaly; Mohamed A Metwally
Journal:  Eur J Med Chem       Date:  2010-05-15       Impact factor: 6.514

7.  New pyrazole derivatives containing 1,2,4-triazoles and benzoxazoles as potent antimicrobial and analgesic agents.

Authors:  A M Vijesh; Arun M Isloor; Prashanth Shetty; S Sundershan; Hoong Kun Fun
Journal:  Eur J Med Chem       Date:  2013-01-10       Impact factor: 6.514

8.  Synthesis, characterization and biological activities of some new benzo[b]thiophene derivatives.

Authors:  Arun M Isloor; Balakrishna Kalluraya; K Sridhar Pai
Journal:  Eur J Med Chem       Date:  2009-11-11       Impact factor: 6.514

9.  Convenient access to 1,3,4-trisubstituted pyrazoles carrying 5-nitrothiophene moiety via 1,3-dipolar cycloaddition of sydnones with acetylenic ketones and their antimicrobial evaluation.

Authors:  N Satheesha Rai; Balakrishna Kalluraya; B Lingappa; Shaliny Shenoy; Vedavati G Puranic
Journal:  Eur J Med Chem       Date:  2007-08-30       Impact factor: 6.514

10.  Crystal structure refinement with SHELXL.

Authors:  George M Sheldrick
Journal:  Acta Crystallogr C Struct Chem       Date:  2015-01-01       Impact factor: 1.172

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.