888944-30-7

Upstream product

• 623-00-7 4-bromobenzenecarbonitrile 
• 189819-75-8 4-amino-1-(t-butoxycarbonyl)piperidine monohydrochloride 
• 1044183-50-7 4-(benzylidene-amino)-piperidine-1-carboxylic acid tert-butyl ester 
• 1029643-92-2 N-phenylmethylidenepiperidinyl-4-amine 
• 13035-19-3 4-aminopiperidine 
• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 
• 105-07-7 4-cyanobenzaldehyde 

Downstream Products

• 888944-31-8 C₃₀H₃₉N₃O₃ 
• 1401532-99-7 C₂₂H₂₀ClN₃OS 
• 1401533-00-3 C₂₂H₁₉Cl₂N₃OS 
• 1401533-01-4 C₂₂H₁₉ClFN₃OS 
• 1401533-17-2 C₂₇H₂₈ClN₃O₃S 
• 1401533-18-3 C₂₇H₂₇Cl₂N₃O₃S 
• 1401533-19-4 C₂₇H₂₇ClFN₃O₃S 
• 1091682-29-9 [1-((S)-2-amino-3,3-dimethyl-butyryl)-piperidin-4-yl]-(4-cyano-benzyl)-carbamic acid benzyl ester hydrochloride 
• 1091682-28-8 (R)-N-{(S)-1-[4-(4-cyano-benzylamino)-piperidine-1-carbonyl]-2,2-dimethyl-propyl}-2-cyclopentylmethyl-3-(formyl-hydroxy-amino)-propionamide 

Relevant academic research and scientific papers

Accessing Aliphatic Amines in C-C Cross-Couplings by Visible Light/Nickel Dual Catalysis

A general aminoalkylation of aryl halides was developed, overcoming intolerance of free amines in nickel-mediated C-C coupling. This transformation features broad functional group tolerance and high efficiency. Taking advantage of the fast desilylation of α-silylamines upon single-electron transfer (SET) facilitated by carbonate, α-amino radicals are generated regioselectively, which then engage in nickel-mediated C-C coupling. The reaction displays high chemoselectivity for C-C over C-N bond formation. Highly functionalized pharmacophores and peptides are also amenable.

Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria

We have previously reported amidopiperidine derivatives as a novel peptide deformylase (PDF) inhibitor and evaluated its antibacterial activity against Gram-positive bacteria, but poor pharmacokinetic profiles have resulted in low efficacy in in vivo mouse models. In order to overcome these weaknesses, we newly synthesized aminopiperidine derivatives with remarkable antimicrobial properties and oral bioavailability, and also identified their in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE) and penicillin-resistant Streptococcus pneumoniae (PRSP).

Potent small molecule Hedgehog agonists induce VEGF expression in vitro

Here, we describe the synthesis, SAR studies as well as biological investigations of the known Hedgehog signaling agonist SAG and a small library of its analogues. The SAG and its derivatives were analyzed for their potency to activate the expression of the Hh target gene Gli1 in a reporter gene assay. By analyzing SAR important molecular descriptors for Gli1 activation have been identified. SAG as well as compound 10c proven to be potent activators of VEGF expression in cultivated dermal fibroblasts. Importantly and in contrast to SAG, derivative 10c displayed no toxicity in concentrations up to 250 μm.

Novel 4-Aminopiperidine Derivatives

Novel substituted 4-aminopiperidine derivatives of the formula I: wherein n, R1, Y, and are as defined in claim 1, and optically pure enantiomers, mixtures of enantiomers, racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates and meso-forms, as well as salts and solvent complexes of such compounds, and morphological forms, that exhibit useful parasite aspartic proteases inhibiting properties and can thus be used in the form of pharmaceutical compositions as antimalarial medicines.