We report an efficient, highly selective modification on the N-terminal amines of peptides and proteins using aldehyde derivatives via reductive alkylation. After modification of a library of unprotected peptides XYSKEASAL (X varies over 20 natural amino acids) by benzaldehyde at room temperature, pH 6.1 resulted in excellent N-terminal selectivity (α-amino/ε-amino: >99 : 1) and high reaction c...

The alkylation of the specific higher-order nucleic acid structures is of great significance in order to control its function and gene expression. In this report, we have described the T-T mismatch selective alkylation with a vinyldiaminotriazine (VDAT)-acridine conjugate. The alkylation selectively proceeded at the N3 position of thymidine on the T-T mismatch. Interestingly, the alkylated thym...

Alkyl derivatives of MEA are used in the production of surfactants, dyes, in the manufacture of drugs as a buffer substance and for the stabilization of emulsions, in the manufacture of herbicides, cosmetics, antihistamines, are also of practical interest [1]. It is widely known also as useful “acid” gases (H2S, CO2, SO2, etc.) as absorbents in the process of cleaning process for gases in oil r...

Alkyl derivatives of MEA are used in the production of surfactants, dyes, in the manufacture of drugs as a buffer substance and for the stabilization of emulsions, in the manufacture of herbicides, cosmetics, antihistamines, are also of practical interest [1]. It is widely known also as useful “acid” gases (H2S, CO2, SO2, etc.) as absorbents in the process of cleaning process for gases in oil r...

Key studies defining the DNA alkylation properties and selectivity of a new class of exceptionally potent, naturally occurring antitumor antibiotics including CC-1065, duocarmycin A, and duocarmycin SA are reviewed. Recent studies conducted with synthetic agents containing deep-seated structural changes and the unnatural enantiomers of the natural products and related analogs have defined the s...

The selective N-4 alkylation of cytosine plays a critical role in the synthesis biologically active molecules. This work focuses on development practical reaction conditions toward regioselective N-4-alkyl derivatives. sequence includes direct and sulfonylation at N-1 site cytosine, followed by amino using KHMDS CH2Cl2/THF mixture, providing fast efficient approach consistent with pyrimidine-ba...

Solvents and catalysts for organic reactions:  Friedel-Crafts reactions,  Alkylation,  Izomerisation,  Acylation,  Esterification,  Cracking,  Diels-Alder addition,  Wittig reactions,  Polymerisation. Solvents in separation processes:  Extraction of metals and organic compounds,  Nuclear wastewater treatment,  Production of selective liquid membranes and sensors. Others:...

An efficient synthesis of a highly potent and selective IP (PGI(2) receptor) agonist that is not structurally analogous to PGI(2) is described. This synthesis is accomplished through the following key steps: Nucleophilic ring-opening of 3-(4-chlorophenyl)-oxazolidin-2-one prepared by a one-pot procedure with 4-piperidinol and selective O-alkylation of 1-(2-(4-chlorophenylamino)ethyl)piperidin-4...