- Rapid, Stoichiometric, Site-Specific Modification of Aldehyde-Containing Proteins Using a Tandem Knoevenagel-Intra Michael Addition Reaction
-
A site-specific modification of aldehyde-containing proteins using a tandem Knoevenagel-intra Michael addition reaction was developed. The reaction featured fast kinetics (50 M-1 s-1) and favorable stoichiometry. Various functionalities could be introduced into the protein with little impact on its function and conformation. The reaction was successfully applied in the labeling of living cells.
- Yu, Jian,Shen, Da,Zhang, Hanjie,Yin, Zheng
-
p. 1016 - 1020
(2018/04/23)
-
- COMPOUNDS AND METHODS FOR PRODUCING A CONJUGATE
-
The present disclosure provides conjugate structures and compound structures used to produce these conjugates. Also provided are methods of producing drug-polypeptide or detectable label-polypeptide conjugates linked through a modified amino acid. Structures of the modified amino acids used in producing the conjugates are disclosed.
- -
-
-
- Intramolecular N-H, O-H, and S-H Insertion Reactions. Synthesis of Heterocycles from α-Diazo β-Keto Esters
-
Several aspects of the Rh2(OAc)4-catalyzed intramolecular N-H, O-H, and S-H insertion reactions have been studied.Examination of the effect of ring size revealed that four-, five- and six-membered nitrogen heterocycles can be efficiently prepared from the corresponding α-diazo β-keto ester precursors (9a-c), whereas competing C-H insertion prevented formation of the seven-membered heterocycle.Variations in solvent, temperature, and catalyst concentration were found to play an important role in determining the product distribution in the cyclization of the 6-carbamoyl 2-diazo 3-keto ester 9c.The intramolecular X-H insertion reaction has also been successful in the synthesis of oxygen (39) and sulfur (49) heterocycles as well as a heterocycle containing two (N, O) heteroatoms (34).
- Moyer, Mikel P.,Feldman, Paul L.,Rapoport, Henry
-
p. 5223 - 5230
(2007/10/02)
-