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Molbank, Volume 2021, Issue 1

2021 March - 22 articles

Cover Story: Here, we describe the synthesis and characterization of N-(6-chloro-3-nitropyridin-2-yl)5-(1-methyl-1H-pyrazol-4-yl)isoquinolin-3-amine. This compound was designed as an irreversible inhibitor of the monopolar spindle 1 kinase (MPS1 or TTK), a promising anticancer target. MPS1 harbors a poorly conserved cysteine in the middle hinge region, which we aimed to address with a reactive warhead relying on nucleophilic aromatic substitution (SNAr) chemistry. While the title compound did not show the expected MPS1 inhibition, mid-nanomolar potency on the kinase p70S6Kβ (S6K2) was observed, offering a new starting point to target this under-investigated enzyme. View this paper.
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Articles (22)

  • Short Note
  • Open Access
2 Citations
9,105 Views
6 Pages

3-(tert-Butyl)-N-(4-methoxybenzyl)-1-methyl-1H-pyrazol-5-amine

  • Diana Becerra,
  • Hugo Rojas and
  • Juan-Carlos Castillo

10 March 2021

We reported an efficient one-pot two-step synthesis of 3-(tert-butyl)-N-(4-methoxybenzyl)-1-methyl-1H-pyrazol-5-amine 3 in good yield by a solvent-free condensation/reduction reaction sequence starting from 3-(tert-butyl)-1-methyl-1H-pyrazol-5-amine...

  • Short Note
  • Open Access
3 Citations
5,997 Views
6 Pages

5-(4-Fluorophenyl)-3-(naphthalen-1-yl)-1-phenyl-1H-pyrazole

  • Jasril Jasril,
  • Neni Frimayanti,
  • Yuana Nurulita,
  • Adel Zamri,
  • Ihsan Ikhtiarudin and
  • Guntur Guntur

10 March 2021

A new fluorinated pyrazole, 5-(4-fluorophenyl)-3-(naphthalen-1-yl)-1-phenyl-1H-pyrazole was successfully synthesized via a two-step reaction. Firstly, the synthesis of pyrazoline was performed via one-pot three-component reaction under microwave irra...

  • Communication
  • Open Access
8 Citations
5,116 Views
10 Pages

Synthesis of 1,5-Disubstituted Tetrazoles in Aqueous Micelles at Room Temperature

  • Mohammed Abdessalam,
  • Madjid Ait Sidhoum,
  • Fatima-Zohra Zradni and
  • Hocine Ilikti

9 March 2021

The ongoing study is a Ugi-azide four-component reaction for the synthesis of 1,5-disubstituted tetrazole(1,5-DST), which involves an aldehyde, different amines, isocyanides, and as azide’s source the Trimethylsilylazide (TMSN3), in water as solvent...

  • Short Note
  • Open Access
4,369 Views
11 Pages

(E)-4-(3-(3-(4-Methoxyphenyl)acryloyl)phenoxy)butyl 2-Hydroxybenzoate

  • Ihsan Ikhtiarudin,
  • Rahma Dona,
  • Neni Frimayanti,
  • Rahayu Utami,
  • Emma Susanti,
  • Mentari Mentari,
  • Nurmaida Nurmaida,
  • Nesa Agistia,
  • Noval Herfindo and
  • Adel Zamri

9 March 2021

A new hybrid compound of chalcone-salicylate (title compound) has been successfully synthesized using a linker mode approach under reflux condition. The structure of the title compound has been established by spectroscopic analysis including UV-Vis,...

  • Short Note
  • Open Access
4 Citations
3,703 Views
8 Pages

(Z)-5-(3′,4′-Bis(benzyloxy)benzylidene)furan-2(5H)-one

  • Angelica Artasensi,
  • Giovanna Baron,
  • Giulio Vistoli,
  • Giancarlo Aldini and
  • Laura Fumagalli

28 February 2021

Over the years secondary metabolites have been considered as lead molecules both in their natural form and as templates for medicinal chemistry. Some secondary metabolites such as polyphenols and flavan-3-ols exert beneficial effects after a modifica...

  • Short Note
  • Open Access
4,305 Views
7 Pages

24 February 2021

Ethyl 4-(butylamino)-3-nitrobenzoate upon “one-pot” nitro-reductive cyclization using sodium dithionite and substituted aldehyde in dimethyl sulphoxide affords ethyl 1-butyl-2-(2-hydroxy-4-methoxyphenyl)-1H-benzo[d]imidazole-5-carboxylate in an 87% y...

  • Communication
  • Open Access
22 Citations
5,521 Views
7 Pages

4 February 2021

Three new Schiff bases of isoniazid were synthesized using microwave-assisted synthesis and conventional condensation with aromatic aldehydes. Synthesized compounds were characterized using elemental analysis, IR, NMR, and Mass spectroscopy. Synthesi...

  • Communication
  • Open Access
1 Citations
3,273 Views
7 Pages

Tetramethyl 1,1′-(2-[{4,5-bis(Methoxycarbonyl)-1H-1,2,3-triazol-1-yl}methyl]-2-[(4-methylphenyl)sulfonamido]propane-1,3-diyl)bis(1H-1,2,3-triazole-4,5-dicarboxylate)

  • Serigne Abdou Khadir Fall,
  • Sara Hajib,
  • Oumaima Karai,
  • Younas Aouine,
  • Salaheddine Boukhssas,
  • Hassane Faraj and
  • Anouar Alami

31 January 2021

A new compound tetramethyl 1,1′-(2-[{4,5-bis(methoxycarbonyl)-1H-1,2,3-triazol-1-yl}methyl]-2-[(4-methylphenyl)sulfonamido]propane-1,3-diyl)bis(1H-1,2,3-triazole-4,5-dicarboxylate) (3) was prepared in two steps starting from 2-((4-methylphenyl)...

  • Short Note
  • Open Access
5 Citations
3,374 Views
4 Pages

(E)-3-(4-Chlorophenyl)-1-(2-fluoro-4-methoxyphenyl)-2-propen-1-one

  • Nicholas Bailey,
  • Alaina Atanes and
  • Bradley O. Ashburn

25 January 2021

Natural products known as chalcones show promise as chemotherapeutic agents for the neglected tropical disease known as leishmaniasis. Our objective is to synthesize new targets of opportunity that may lead to better treatments of this debilitating d...

  • Short Note
  • Open Access
1 Citations
2,868 Views
5 Pages

21 January 2021

A new thiophene-substituted terpyridine derivative has been prepared through the reaction between 5-n-propylthiophene-2-carboxaldehyde and 2-acetylpyridine. This terpyridine derivative bears an alkyl chain linked via a thiophene heterocycle.

  • Short Note
  • Open Access
5 Citations
5,567 Views
6 Pages

N-(6-Chloro-3-nitropyridin-2-yl)-5-(1-methyl-1H-pyrazol-4-yl)isoquinolin-3-amine

  • Valentin Wydra,
  • Stefan Gerstenecker,
  • Dieter Schollmeyer,
  • Stanislav Andreev,
  • Teodor Dimitrov,
  • Ricardo Augusto Massarico Serafim,
  • Stefan Laufer and
  • Matthias Gehringer

18 January 2021

Here we describe the synthesis of N-(6-chloro-3-nitropyridin-2-yl)5-(1-methyl-1H-pyrazol-4-yl)isoquinolin-3-amine via a three-step procedure including a Buchwald–Hartwig arylamination with benzophenone imine and a highly regioselective nucleoph...

  • Short Note
  • Open Access
1 Citations
2,673 Views
5 Pages

Cis-Bis(2,2′-Azopyridinido)dicarbonylruthenium(II)

  • Tsugiko Takase,
  • Shuya Kainuma,
  • Takatoshi Kanno and
  • Dai Oyama

18 January 2021

An [Ru(apy)2Cl2] precursor (apy = 2,2′-azopyridine) in 2-methoxyethanol was heated under a pressurized CO atmosphere to afford a diradical complex, [Ru(apy·)2(CO)2], containing one-electron-reduced azo anion radical ligands. The e...

  • Communication
  • Open Access
7 Citations
4,015 Views
5 Pages

Unexpected Metal-Free Dehydrogenation of a β-Ketoester to a Phenol Using a Recyclable Oxoammonium Salt

  • Fabrizio Politano,
  • William P. Brydon,
  • Jyoti Nandi and
  • Nicholas E. Leadbeater

13 January 2021

The conversion of ethyl 2-oxocyclohexanecarboxylate to ethyl salicylate using an oxoammonium salt is reported. The dehydrogenation reaction is operationally simple and compares favorably with previous literature examples for the same transformation a...

  • Communication
  • Open Access
5 Citations
4,658 Views
9 Pages

Synthesis and Structural Characterization of (E)-4-[(2-Hydroxy-3-methoxybenzylidene)amino]butanoic Acid and Its Novel Cu(II) Complex

  • Eleftherios Halevas,
  • Antonios Hatzidimitriou,
  • Barbara Mavroidi,
  • Marina Sagnou,
  • Maria Pelecanou and
  • Dimitris Matiadis

6 January 2021

A novel Cu(II) complex based on the Schiff base obtained by the condensation of ortho-vanillin with gamma-aminobutyric acid was synthesized. The compounds are physico-chemically characterized by elemental analysis, HR-ESI-MS, FT-IR, and UV-Vis. The c...

  • Short Note
  • Open Access
1 Citations
2,957 Views
4 Pages

(S)-1-(Ethoxycarbonyl)ethyl(2R,5S)-2,5-dimethyl-1,3-dioxolan-4-one-2-carboxylate

  • R. Alan Aitken,
  • Oliver E. Haslett and
  • Alexandra M. Z. Slawin

2 January 2021

The title compound was obtained in low yield in the condensation of ethyl pyruvate and lactic acid. Its structure is determined by NMR methods and x-ray diffraction and the mechanism for formation of this 1:2 adduct from the initial 1:1 adduct is con...

  • Short Note
  • Open Access
3,496 Views
4 Pages

N-(2-(1H-Indol-3-yl)ethyl)-2-(2-fluoro-[1,1′-biphenyl]-4-yl)propanamide

  • Stanimir Manolov,
  • Iliyan Ivanov and
  • Dimitar Bojilov

31 December 2020

N-(2-(1H-Indol-3-yl)ethyl)-2-(2-fluoro-[1,1′-biphenyl]-4-yl)propanamide was prepared by a reaction between tryptamine and flurbiprofen, applying N,N’-Dicyclohexylcarbodiimide, as a coupling agent. The obtained new amide has a fragment similar to Breq...

  • Short Note
  • Open Access
1 Citations
3,169 Views
4 Pages

Methyl (2E)-3-[3-Benzyl-2-(3-methoxy-3-oxoprop-1-yn-1-yl)-2-(1-naphthyl)imidazolidin-1-yl]acrylate

  • Alexandra S. Golubenkova,
  • Nikita E. Golantsov and
  • Leonid G. Voskressensky

30 December 2020

Compounds with propargylamine moiety are useful synthetic precursors of several important classes of nitrogen-containing heterocycles. The title compound, methyl (2E)-3-[3-benzyl-2-(3-methoxy-3-oxoprop-1-yn-1-yl)-2-(1-naphthyl)imidazolidine-1-yl]acry...

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Molbank - ISSN 1422-8599