58644-54-5

Usage

Chemical Properties

Oil

Uses

Inhibitor of Human Alcohol Dehydrogenase enzyme.

Upstream product

• 107-31-3 Methyl formate 
• 765-30-0 Cyclopropylamine 
• 124-38-9 carbon dioxide 
• 68-12-2 N,N-dimethyl-formamide 
• 64-18-6 formic acid 
• 109-94-4 formic acid ethyl ester 

Downstream Products

• 58644-53-4 cyclopropyl isocyanide 
• 1262043-90-2 benzyl (6-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)carbamate 
• 86483-53-6 3-Cyclopropylamino-2-(2,4-dichlor-5-fluorbenzoyl)acrylsaeure-ethylester 
• 856707-38-5 acetic acid (2S)-2-tert-butoxycarbonylamino-1-cyclopropylcarbamoylpentyl ester 
• 246257-66-9 benzylcyclopropylformamide 
• 67376-94-7 methylcyclopropylamine hydrochloride 

Relevant academic research and scientific papers

A substituent- And temperature-controllable NHC-derived zwitterionic catalyst enables CO2upgrading for high-efficiency construction of formamides and benzimidazoles

Chemocatalytic upgrading of the greenhouse gas CO2 to valuable chemicals and biofuels has attracted broad attention in recent years. Among the reported approaches, N-formylation of CO2 with an amine is of great significance due to its versatility in the construction of N-containing linear and cyclic skeletons. Herein, a stable N-heterocyclic carbene-carboxyl adduct (NHC-CO2) was facilely prepared and could be used as a recyclable zwitterionic catalyst for efficient CO2 reductive upgrading via either N-formylation or further coupling with cyclization under mild conditions (25 °C, 1 atm CO2) using hydrosilane as a hydrogen source. More than 30 different alkyl and aromatic amines could be transformed into the corresponding formamides or benzimidazoles with remarkable yields (74%-98%). The electronic effect of the introduced substituent on NHC-CO2 was found to evidently affect the thermostability and nucleophilicity of the zwitterionic catalyst, which is directly correlated with its catalytic activity. Moreover, NHC-CO2 could supply CO2 by in situ decarboxylation at a specific temperature that is dependent on the introduced substituent type. Experimental and computational studies showed that the carboxyl species on NHC-CO2 was not only a nucleophilic center, but also a C1 source which rapidly captures or substitutes ambient CO2 during hydrosilylation. In addition, a simple and green conceptual process was designed for the product purification and catalyst recycling, with a good feasibility for small-scale production.

TRIAZOLONES DERIVATIVES FOR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE

The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, codrug, cocrystal, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Formamide Synthesis through Borinic Acid Catalysed Transamidation under Mild Conditions

A highly efficient and mild transamidation of amides with amines co-catalysed by borinic acid and acetic acid has been reported. A wide range of functionalised formamides was synthesized in excellent yields, including important chiral α-amino acid derivatives, with minor racemisation being observed. Experiments suggested that the reaction rely on a cooperative catalysis involving an enhanced boron-derived Lewis acidity rather than an improved Br?nsted acidity of acetic acid. Amide bonds are reputedly difficult to activate due to their high resonance stabilization. An unusual mild activation of dimethylformamide and formamide by borinic acid 1 (see scheme), illustrated by a general formylation of a wide range of amines, including chiral α-amino esters, has been reported.

Pyrroloquinoline Derivatives And Their Use As Protein Kinases Inhibitors

The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.

Deuterated hepatitis C protease inhibitors

A deuterated α-ketoamido steric specific compound of the formula wherein D denotes a deuterium atom on a steric specific carbon atom.

QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS

The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Inhibition of human alcohol dehydrogenases by formamides

Human alcohol dehydrogenase (HsADH) comprises class I (α, β, and γ), class II (π), and class IV (σ) enzymes. Selective inhibitors of the enzymes could be used to prevent the metabolism of alcohols that form toxic products. Formamides are unreactive analog

Selective κ-opioid agonists: Synthesis and structure-activity relationships of piperidines incorporating an oxo-containing acyl group

This study describes the synthesis and the structure-activity relationships (SARs) of the (S)-(-)-enantiomers of a novel class of 2- (aminomethyl)piperidine derivatives, using κ-opioid binding affinity and antinociceptive potency as the indices of biological activity. Compounds incorporating the 1-tetralon-6-ylacetyl residue (30 and 34-45) demonstrated an in vivo antinociceptive activity greater than predicted on the basis of their κ-binding affinities. In particular, (2S)-2-[(dimethylamino)methyl]- 1-[(5,6,7,8-tetrahydro-5-oxo-2-naphthyl)acetyl]piperidine (34) was found to have a potency similar to spiradoline in animal models of antinociception after subcutaneous administration, with ED50s of 0.47 and 0.73 μmol/kg in the mouse and in the rat abdominal constriction tests, respectively. Further in vivo studies in mice and/or rats revealed that compound 34, compared to other selective κ-agonists, has a reduced propensity to cause a number of κ-related side effects, including locomotor impairment/sedation and diuresis, at antinociceptive doses. For example, it has an ED50 of 26.5 μmol/kg sc in the rat rotarod model, exhibiting a ratio of locomotor impairment/sedation vs analgesia of 36. Possible reasons for this differential activity and its clinical consequence are discussed.

N-Alkyl-N-iminomethyl derivatives of thienamycin

Disclosed are N-alkyl-N-iminomethyl derivatives of thienamycin which may be represented by the following structural formula: STR1 wherein R5 is, inter alia, alkyl, alkenyl, aryl, or aralkyl, R6 is selected from R, OR, SR and NR1