333366-23-7

Usage

Uses

Used in Pharmaceutical Industry:
N3-Asp(tBu)-OH (dicyclohexylammonium) salt is used as a reagent for the preparation of acyclic nucleoside phosphonates containing 0-deazahypoxanthine. These compounds are crucial in the development of drugs that target and inhibit plasmodial 6-oxopurine phosphoribosyltransferases, which are essential enzymes in the survival and replication of Plasmodium parasites responsible for malaria. By inhibiting these enzymes, the acyclic nucleoside phosphonates can effectively combat malaria and related diseases.

Upstream product

• 3057-74-7 L-Asp(t-Bu) 

Downstream Products

• 1189342-34-4 tert-butyl (S)-3-azido-4-oxo-4-{[3-(triisopropylsilyl)-prop-2-ynyl]amino}butanoate 
• 103060-53-3 daptomycin 

Relevant academic research and scientific papers

BENZODIAZEPINES AS BROMODOMAIN INHIBITORS

The present invention provides novel benzodiazepine derivatives of Formula I or pharmaceutically acceptable derivatives, polymorphs, salts or prodrugs thereof. Said compounds have potential as bromodomain (BRD) inhibitors.

Synthesis of a biologically active triazole-containing analogue of cystatin A through successive peptidomimetic alkyne-azide ligations

"Click" protein: CuI-catalyzed cycloaddition of azides and terminal alkynes has been applied to the successive ligations of three unprotected peptide fragments. Peptidomimetic triazole ligation (PTL, see scheme) as a new method for the chemical production of bioactive proteins is applied for the synthesis of a triazole-containing analogue of the 97 amino acid protein cystatin A. Copyright

Solid-phase Staudinger ligation from a novel core-shell-type resin: A tool for facile condensation of small peptide fragments

Solid-phase Staudinger ligation of small peptides was performed on a novel core-shell-type resin. Solid-phase Staudinger ligation was mediated by synthetic solid-supported phosphinothiol, which was readily prepared by a straightforward synthetic route. This protocol afforded final peptide products in excellent yields and purities and thus could provide the opportunity to facilitate a simple manipulation for condensation of peptide fragments. In particular, the resulting resin could be recycled in a successful manner.

Improved solid-phase peptide synthesis method utilizing alpha-azide-protected amino acids.

[structure: see text]. Pure alpha-azido acids were prepared using an efficient diazo transfer method followed by buffered workup. These building blocks were used to prepare small peptides on Wang resin by two approaches. Peptides prone to diketopiperazine formation were prepared in good yields by coupling acids to resin bound iminophosphoranes during Fmoc-Wang synthesis. The iminophosphoranes can also be hydrolyzed under neutral conditions to provide unprotected amines ready for further coupling.