73724-40-0Relevant articles and documents
NEODEGRADER CONJUGATES
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Paragraph 0580; 0610, (2021/10/11)
The present disclosure provides neoDegraders and neoDegraders conjugated to binding moieties. Also provided are compositions comprising the conjugates. The compounds and compositions are useful for treating a disease or condition, e.g., cancer, in a subject in need thereof.
Fmoc-AA-NH2 Preparation method
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Paragraph 0049-0050, (2021/10/02)
The invention relates to Fmoc-AA-NH. 2 The invention discloses a preparation method of a polypeptide and belongs to the technical field of polypeptide synthesis. Fmoc-AA-NH of the present invention2 The preparation method comprises: NH. 4 X Is first dissolved in a basic solvent system, and then Fmoc-AA-OSu reaction is added to obtain Fmoc-AA-NH. 2 . Wherein, pH of the reaction is 8 - 9, and AA is an amino acid or an amino acid derivative with only one carboxyl group. NH4 X Is NH. 4 Cl, (NH4)2 SO4 At least one of the foregoing. The base in the basic solvent system is NaHCO. 3 , KHCO3 , Na2 CO3 , K2 CO3 At least one of the foregoing. The solvent system in the alkaline solvent system is THF/H. 2 O, CAN / H2 At least one of O.
Ynamide-Mediated Thiopeptide Synthesis
Yang, Jinhua,Wang, Changliu,Xu, Silin,Zhao, Junfeng
supporting information, p. 1382 - 1386 (2019/01/08)
Exploration of the full potential of thioamide substitution as a tool in the chemical biology of peptides and proteins has been hampered by insufficient synthetic strategies for the site-specific introduction of a thioamide bond into a peptide backbone. A novel ynamide-mediated two-step strategy for thiopeptide bond formation with readily available monothiocarboxylic acids as thioacyl donors is described. The α-thioacyloxyenamide intermediates formed from the ynamides and monothiocarboxylic acids can be purified, characterized, and stored. The balance between their activity and stability enables them to act as effective thioacylating reagents to afford thiopeptide bonds under mild reaction conditions. Amino acid functional groups such as OH, CONH2, and indole NH groups need not be protected during thiopeptide synthesis. The modular nature of this strategy enables the site-specific incorporation of a thioamide bond into peptide backbones in both solution and the solid phase.