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TCI Chemistry News

January 2023

 

TCI offers an extensive catalog of 31,000 high quality organic reagents suitable for benchtop-to-bulk chemistry. This issue covers our chemistry topics as follows:

  • Non-PEG Linkers for Designing Proteolysis Targeting Chimera Molecules
  • The Intermolecular [2+2] Cycloaddition Catalyzed by a Photoredox Catalyst
  • Regioselective Acylation of a Carbohydrate Utilizing the Benzoxaborole Catalyst
  • TCI Chemistry Research: TCIMAIL 191
Non-PEG Linkers for Designing Proteolysis Targeting Chimera Molecules

Non-PEG Linkers for Designing Proteolysis Targeting Chimera Molecules

Proteolysis targeting chimera molecules are bifunctional small molecules which consist of a ubiquitin E3 ligase ligand and a protein of interest (POI) ligand covalently bonded via a linker. The chimera molecules that induce the degradation of POI, while conventional molecules cannot, are regarded as a new drug modality. Although PEG linkers are typically used as linkers, the drug-like structures using non-PEG linkers with shorter linker length have been recently reported. Non-PEG linkers, 1-Boc-4-(piperidin-4-ylmethyl)piperazine [D5965] and 1-Boc-4-(piperazin-1-ylmethyl)piperidine [D5966] can bind to various ligands. The proteolysis targeting chimera molecules derivatized from D5965 or D5966 are studied as potential oral drugs.

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The Intermolecular [2+2] Cycloaddition Catalyzed by a Photoredox Catalyst

TCI Practical Example: The Intermolecular [2+2] Cycloaddition Catalyzed by a Photoredox Catalyst

TCI introduces the [2+2] photocycloaddition reaction between ethyl (E)-4-(4-fluorophenyl)-2-oxobut-3-enoate and 1,1-diphenylethylene catalyzed by Ru(phen)3(PF6)2 [T3208]. You can see many photoredox catalysts in TCI product brochure.

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Regioselective Acylation of a Carbohydrate Utilizing the Benzoxaborole Catalyst

TCI Practical Example: Regioselective Acylation of a Carbohydrate Utilizing the Benzoxaborole Catalyst

We are proud to present the 3-position-selective benzoylation of methyl α-L-fucopyranoside catalyzed by the benzoxaborole derivative [F1259]. TCI has various monosaccharides and carbohydrate building blocks for the synthesis of carbohydrate derivatives.

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TCIMAIL 191

TCI Chemistry Research: TCIMAIL 191

Released in December 2022, TCI's latest issue features Prof. Emerit. Shin-ichiro Shoda’s article and Prof. Nagatoshi Nishiwaki’s chemistry chat. We also feature research on:

  • Visible Light Photoredox Catalyst for Decarboxylation Reactions
  • Racemization-Free Ynamide-Type Condensing Agent
  • Azetidine-Containing Tertiary Boronic Acid Esters
  • p-Sexiphenyl for the Improvement of OFET
  • Methacrylamide with TMP Group as a Side Chain
  • “Non-Fucosyl G2 N-Glycan” Expected as a High-Functional Glycoform for Therapeutic Antibody
  • Phosphodiesterase Inhibitor
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