Convenient Synthesis of Alternatively Bridged Tryptophan Ketopiperazines and their Activities Against Trypanosomatid Parasites

ChemMedChem ◽  
2021 ◽  
Author(s):  
Peter E. Cockram ◽  
Callum Turner ◽  
Alexandra M. Z. Slawin ◽  
Terry Smith
Keyword(s):  
Convenient Synthesis ◽  
Trypanosomatid Parasites

Convenient Synthesis of (Z)-7- and (E)-9-dodecene-1-yl Acetate, Components of Some Lepidoptera Insect Sex Pheromone

2017 ◽  
Vol 68 (1) ◽  
pp. 180-185
Author(s):  
Adriana Maria Andreica ◽  
Lucia Gansca ◽  
Irina Ciotlaus ◽  
Ioan Oprean
Keyword(s):  
Sex Pheromone ◽  
Coupling Reaction ◽  
Coupling Scheme ◽  
Lithium Aluminium Hydride ◽  
Terminal Alkyne ◽  
Mercury Derivative ◽  
Lithium Aluminium ◽  
Convenient Synthesis ◽  
Practical Synthesis ◽  
Insect Sex

Were developed new and practical synthesis of (Z)-7-dodecene-1-yl acetate and (E)-9-dodecene-1-yl acetate. The routes involve, as the key step, the use of the mercury derivative of the terminal-alkyne w-functionalised as intermediate. The synthesis of (Z)-7-dodecene-1-yl acetate was based on a C6+C2=C8 and C8+C4=C12 coupling scheme, starting from 1,6-hexane-diol. The first coupling reaction took place between 1-tert-butoxy-6-bromo-hexane and lithium acetylide-ethylendiamine complex obtaining 1-tert-butoxy-oct-7-yne, which is transformed in di[tert-butoxy-oct-7-yne]mercury. The mercury derivative was directly lithiated and then alkylated with 1-bromobutane obtaining 1-tert-butoxy-dodec-7-yne. After acetylation and reduction with lithium aluminium hydride of 7-dodecyne-1-yl acetate gave (Z)-7-dodecene-1-yl acetate with 96 % purity. The synthesis of (E)-9-dodecene-1-yl acetate was based on a C8+C2=C10 and C10+C2=C12 coupling scheme, starting from 1,8-octane-diol. The first coupling reaction took place between 1-tert-butoxy-8-bromo-octane and lithium acetylide-ethylendiamine complex obtaining 1-tert-butoxy-dec-9-yne, which is transformed in di[tert-butoxy-dec-9-yne]mercury. The mercury derivative was directly lithiated and then alkylated with 1-bromoethane obtaining 1-tert-butoxy-dodec-9-yne. After reduction with lithium aluminium hydride of 1-tert-butoxy-(E)-9-dodecene and acetylation was obtained (E)-9-dodecene-1-yl acetate with 97 % purity.

Cysteine Peptidase Inhibitors in Trypanosomatid Parasites

2013 ◽  
Vol 20 (25) ◽  
pp. 3152-3173 ◽  
Author(s):  
A. Lima ◽  
F. Reis ◽  
T. Costa
Keyword(s):  
Peptidase Inhibitors ◽  
Cysteine Peptidase ◽  
Trypanosomatid Parasites

A New and Convenient Synthesis of the Boceprevir P1 Fragment, ?-amino-?-Hydroxy Amide

2016 ◽  
Vol 13 (5) ◽  
pp. 352-358
Author(s):  
Jayaprakash Rao Yerrabelly ◽  
Pradeep Rebelli ◽  
Bharathi Kumari Yalamanchili ◽  
Venkat Reddy Ghojala
Keyword(s):  
Convenient Synthesis

Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
One Pot ◽  
Triazole Derivatives ◽  
Sar Studies ◽  
Convenient Synthesis ◽  
Antibacterial And Antifungal

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

ChemInform Abstract: A New Route for the Convenient Synthesis of 3-(Thiazol-2′-ylthio)-2H-1-benzopyran-2-ones.

ChemInform ◽  
1987 ◽  
Vol 18 (33) ◽  
Author(s):  
V. K. AHLUWALIA ◽  
H. R. SHARMA ◽  
R. TYAGI
Keyword(s):  
Convenient Synthesis

Convenient Synthesis of the Central 3,6-Di(2-thiazolyl)-2-(4-thiazolyl)pyridine Skeleton of a Macrocyclic Antibiotic, GE 2270 A

1998 ◽  
Vol 71 (8) ◽  
pp. 1863-1870 ◽  
Author(s):  
Kazuo Okumura ◽  
Hiroyuki Saito ◽  
Chung-gi Shin ◽  
Kazuyuki Umemura ◽  
Juji Yoshimura
Keyword(s):  
Macrocyclic Antibiotic ◽  
Convenient Synthesis
Sign in / Sign up

Export Citation Format

Share Document