125342-48-5

Usage

Uses

Used in Biotechnological Applications:
DL-Norleucine, N-[(1,1-dimethylethoxy)carbonyl]is used as a stabilizing and solubilizing agent for peptides and proteins, improving their stability and solubility in various formulations. This enhancement is crucial for the development of more effective and stable pharmaceuticals and biotechnological products.
Used in Pharmaceutical Production:
In the pharmaceutical industry, DL-Norleucine, N-[(1,1-dimethylethoxy)carbonyl]is used as an additive to improve the stability and solubility of peptide and protein-based drugs. This contributes to the development of more effective medications with better pharmacokinetic properties.
Used in Biochemical Research:
DL-Norleucine, N-[(1,1-dimethylethoxy)carbonyl]serves as a valuable tool in biochemical research, where it is used in the synthesis of new and modified amino acids. This allows researchers to explore novel compounds with potential applications in medicine, agriculture, and other fields.
Used in Peptide and Protein Synthesis:
In the synthesis of peptides and proteins, DL-Norleucine, N-[(1,1-dimethylethoxy)carbonyl]is used to improve the yield and quality of the final product. Its ability to enhance stability and solubility makes it an essential component in the development of therapeutic peptides and proteins.
Overall, DL-Norleucine, N-[(1,1-dimethylethoxy)carbonyl]plays a significant role in various industries, including biotechnology, pharmaceuticals, and biochemical research, due to its ability to improve the stability and solubility of peptides and proteins.

Upstream product

• 109-65-9 1-bromo-butane 
• 4530-20-5 BOC-glycine 
• 616-06-8 2-amino-hexanoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 70288-84-5 2-aminohexanoic acid (hydrochloride) 

Downstream Products

• 439287-52-2 (+/-)-2-(tert-butoxycarbonyl)-amino-N-[(2,6-dimethyl)phenyl]hexanamide 
• 120369-42-8 L-N-Boc-norleucine benzylamide 
• 104062-70-6 (1-formyl-pentyl)-carbamic acid tert-butyl ester 
• 367258-50-2 {1-[({[(dimethylcarbamoyl-phenyl-methyl)-carbamoyl]-methyl}-carbamoyl)-hydroxy-methyl]-pentyl}-carbamic acid tert-butyl ester 
• 125342-49-6 [1-(2-Benzyloxycarbonylamino-ethylcarbamoyl)-pentyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Enantioselective Deaminative Alkylation of Amino Acid Derivatives with Unactivated Olefins

Herein, we report the first Ni-catalyzed enantioselective deaminative alkylation of amino acid and peptide derivatives with unactivated olefins. Key for success was the discovery of a new sterically encumbered bis(oxazoline) ligand backbone, thus offering a de novo technology for accessing enantioenriched sp3-sp3 linkages via sp3 C-N functionalization. Our protocol is distinguished by its broad scope and generality across a wide number of counterparts, even in the context of late-stage functionalization. In addition, an enantioselective deaminative remote hydroalkylation reaction of unactivated internal olefins is within reach, thus providing a useful entry point for forging enantioenriched sp3-sp3 centers at remote sp3 C-H sites.

Optimization and Evaluation of Novel Antifungal Agents for the Treatment of Fungal Infection

Due to the increased morbidity and mortality by fungal infections and the emergence of severe antifungal resistance, there is an urgent need for new antifungal agents. Here, we screened for antifungal activity in our in-house library through the minimum inhibitory concentration test and derived two hit compounds with moderate antifungal activities. The hit compounds' antifungal activities and drug-like properties were optimized by substituting various aryl ring, alkyl chain, and methyl groups. Among the optimized compounds, 22h was the most promising candidate with good drug-like properties and exhibited potent fast-acting fungicidal antifungal effects against various fungal pathogens and synergistic antifungal activities with some known antifungal drugs. Additionally, 22h was further confirmed to disturb fungal cell wall integrity by activating multiple cell wall integrity pathways. Furthermore, 22h exerted significant antifungal efficacy in both the subcutaneous infection mouse model and ex vivo human nail infection model.

BENZOTHIA(DI)AZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

UREA DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE

The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis. The derivative is represented by Formula (I): [Chemical formula I] wherein Cy is an aromatic hydrocarbon group which may be substituted or an aromatic heterocyclic group which may be substituted; R1 is a hydrogen atom or a hydrocarbon group which may be substituted; V is -C(O)-, -S(O)-, or -S(O)2-; W is -N(R2)-, -O-, or a bond (wherein R2 is a hydrogen atom or a hydrocarbon group which may be substituted); X is alkylene which may be substituted; Y is -C(O)-, -S(O)-, or -S(O)2-; Z is a bond, a chain hydrocarbon group which may be substituted, or -N=; ring A is a non-aromatic nitrogen-containing heterocyclic ring which may be substituted; ring B is a nitrogen-containing heterocyclic ring which may be substituted; and [Chemical formula 2]------￣?,?------? are each independently a single bond or a double bond; provided that R1 may be bonded to R2 to form a non-aromatic nitrogen-containing heterocyclic ring and that R2 may be bonded to a substituent of X to form a non-aromatic nitrogen-containing heterocyclic ring which may be substituted.

Synthesis and structure-activity relationships of potential anticonvulsants based on 2-piperidinecarboxylic acid and related pharmacophores

Using N-(2,6-dimethyl)phenyl-2-piperidinecarboxamide (1) and N-(α-methylbenzyl)-2-piperidinecarboxamide (2) as structural leads, a variety of analogues were synthesised and evaluated for anticonvulsant activity in the MES test in mice. In the N-benzyl series, introduction of 3-Cl, 4-Cl, 3,4-Cl2, or 3-CF3 groups on the aromatic ring led to an increase in MES activity. Replacement of the α-methyl group by either i-Pr or benzyl groups enhanced MES activity with no increase in neurotoxicity. Substitution on the piperidine ring nitrogen led to a decrease in MES activity and neurotoxicity, while reduction of the amide carbonyl led to a complete loss of activity. Movement of the carboxamide group to either the 3- or 4-positions of the piperidine ring decreased MES activity and neurotoxicity. Incorporation of the piperidine ring into a tetrahydroisoquinoline or diazahydrinone nucleus led to increased neurotoxicity. In the N-(2,6-dimethyl)phenyl series, opening of the piperidine ring between the 1- and 6-positions gave the active norleucine derivative 75 (ED50 = 5.8 mg kg-1, TD50 = 36.4 mg kg-1, PI = 6.3). Replacement of the piperidine ring of 1 by cycloalkane (cyclohexane, cyclopentane, and cyclobutane) resulted in compounds with decreased MES activity and neurotoxicity, whereas replacement of the piperidine ring by a 4-pyridyl group led to a retention of MES activity with a comparable PI. Simplification of the 2-piperidinecarboxamide nucleus of 1 into a glycinecarboxamide nucleus led to about a six-fold decrease in MES activity. The 2,6-dimethylanilides were the most potent compounds in the MES test in each group of compounds evaluated, and compounds 50 and 75 should be useful leads in the development of agents for the treatment of tonic-clonic and partial seizures in man.

Direct synthesis of Boc protected (D,L)-amino acids from Boc-glycine

Boc-glycine is easily deprotonated by lithium diisopropylamide, yielding a trianion which is trapped with an electrophile to give access to Boc-(D,L)-amino acids.

Composition containing a penem or carbapenem antibiotic and the use of the same

Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially.