127977-30-4

Upstream product

• 598-56-1 N,N-dimethyl-ethanamine 
• 123855-66-3 (S)-2-tert-Butoxycarbonylamino-3-phenyl-propionic acid (R)-3-((S)-2-tert-butoxycarbonylamino-3-phenyl-propionylamino)-2-oxo-pyrrolidin-1-yl ester 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 108-00-9 N,N-dimethylethylenediamine 
• 543-27-1 isobutyl chloroformate 

Downstream Products

• 744198-28-5 H-L-Phe-NH(CH₂)2NMe₂ 

Relevant academic research and scientific papers

Highly sensitive determination of amino acids by LC-MS under neutral conditions

Peptide drug leads possess unusual structural features that allow them to exert their unique biological activities and ideal physicochemical properties. In particular, these peptides often have D-amino acids, and therefore the absolute configurations of t

Development and application of highly sensitive labeling reagents for amino acids

Peptide natural products produced by microorganisms have attracted considerable attention as ideal drug leads owing to their low toxicity and high specificity toward target proteins compared with small-sized molecules. These peptide drug leads possess unu

Process for lowering the viscosity of highly concentrated protein solutions

A process of lowering the viscosity of a solution includes preparing a solution comprising a compound of formula I, at a concentration in the final formulation of between 10 and 250 mM, and a protein having at least one antibody fragment whose concentration is between 50 and 350 mg/mL and whose pH is between 5 and 8. The compound lowers the viscosity of the solution, which is difficult to inject, by a value of at least 15% relative to the viscosity of a solution of at least one protein having at least one antibody fragment of the same concentration and of the same pH not containing the compound.

GLYT2 MODULATORS

α-, β-, and γ-amino acid derivatives of formula I are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain. Formula I

Design of an organocatalyst for the enantioselective Diels-Alder reaction with α-acyloxyacroleins

We have realized the first enantioselective organocatalytic Diels-Alder reaction between α-substituted acroleins, such as α-acyloxyacroleins, and not only cyclic but also acyclic dienes. α-Acyloxyacroleins are useful as synthetic equivalents of α-haloacro

Novel glycine transporter type-2 reuptake inhibitors. Part 1: α-amino acid derivatives

A variety of α-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [ 14C]-glycine in COS7 cells transfected with human glycine transporter-2 (hGlyT-2) was evaluated. An array of substituents at the chiral center was studied and overall, L-phenylalanine was identified as the preferred amino acid residue. Compounds prepared from L-amino acids were more potent GlyT-2 inhibitors than analogs derived from the corresponding D-amino acids. Introducing an achiral amino acid such as glycine, or incorporating geminal substitution in the α-position, led to a significant reduction in GlyT-2 inhibitory properties.

Chiral N-acylethylenediamines as new modular ligands for the catalytic asymmetric addition of alkylzinc reagents to aldehydes

Chiral N-acylethylenediamines represent a new class of modular ligands for the catalytic asymmetric addition of alkylzinc reagents to aldehydes. The N-acylethylenediamine moiety serves as a metal binding site, while attached amino acids provide the source of chirality. Three sites of diversity on the ligands were optimized to enhance the enantioselectivity of the catalysts using an iterative optimization procedure. The most effective ligand, 4k, was synthesized in a single reaction step from inexpensive and commercially available starting materials. This ligand (10 mol %) catalyzed the addition of Me2Zn to 2-naphthaldehyde, benzaldehyde, and 4-chlorobenzaldehyde to give the corresponding alcohol products in 86%, 84% and 81% ee, respectively.