214749-90-3

Upstream product

• 917365-39-0 4-(N-(tert-butoxycarbonyl)-2-nitrophenylsulfonamido)but-2-ynyl benzoate 
• 198572-71-3 N-(tert-butoxycarbonyl)-2-nitrobenzenesulfonamide 
• 64244-47-9 4-(tetrahydro-pyran-2-yloxy)-but-2-yn-1-ol 
• 2446-83-5 di-isopropyl azodicarboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 63200-68-0 4-hydroxy-but-2-ynamine 
• 163682-68-6 4-<(methylsulfonyl)oxy>but-2-yn-1-ol 
• 147743-69-9 4-hydroxybut-2-yn-1-yl 4-methylbenzenesulfonate 
• 50-00-0 formaldehyd 
• 92136-39-5 N-tert-Butoxycarbonyl-1-amino-3-propyne 

Downstream Products

• 917365-55-0 C₂₆H₂₉BrN₂O₆S 
• 917365-54-9 C₂₆H₂₉BrN₂O₆S 
• 917365-58-3 C₂₆H₂₇BrN₂O₆S 
• 917365-40-3 4-(tert-butoxycarbonylamino)but-2-ynyl benzoate 
• 81477-94-3 N-(diphenylmethylene)glycine tert-butyl ester 
• 128490-08-4 (E)-tert-butyl (4-hydroxybut-2-en-1-yl)carbamate 

Relevant academic research and scientific papers

NOVEL IMIDAZOPYRAZINE DERIVATIVES

The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein Rx and R3 to R5 are as described herein (formula (I)) or pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

Total Synthesis of ent-Plagiochianin B

An enantioselective total synthesis of plagiochianin B is described that employs (+)-3-carene as its point of departure and delivers the enantiomer of the natural product. Key features of the synthesis include a palladium-mediated regioselective oxidative

Methylation of geometrically constrained lysine analogues by histone lysine methyltransferases

We report synthesis and enzymatic assays on human histone lysine methyltransferase catalysed methylation of histones that possess lysine and its geometrically constrained analogues containing rigid (E)-alkene (KE), (Z)-alkene (KZ) and alkyne (Kyne) moieties. Methyltransferases G9a and GLP do have a capacity to catalyse methylation in the order K ? KE > KZ ～ Kyne, whereas monomethyltransferase SETD8 catalyses only methylation of K and KE,.

Asymmetric Synthesis of Lysine Analogues with Reduced Basicity, and their Incorporation into Proteasome Inhibitors

Most known β2-selective proteasome inhibitors suffer from relatively poor cell permeability as the result of a net positive charge caused by the basic moiety at P1. In this paper, we describe the synthesis of oligopeptide vinyl sulfones that contain different amino acids bearing amino groups with reduced basicity at P1 and/or P3. For this, we developed the first enantioselective synthesis of lysine(4-ene) and lysine(4-yne). These amino acids, as well as histidine and diaminopropionic-acid-glycine, were incorporated at the P1 and/or P3 positions of oligopeptide vinyl sulfones. All inhibitors were found to inhibit β2, but with a loss of potency compared to our most potent and selective β2 inhibitor, LU-102. These results notwithstanding, our results provide important insights for the future design of β2-selective proteasome inhibitors.

Progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein- mediated multidrug efflux: Design, synthesis, characterization and biological evaluation

Bivalent ligands were designed on the basis of the described close proximity of the ATP-site and the putative steroid-binding site of P-glycoprotein (ABCB1). The syntheses of 19 progesterone-adenine hybrids are described. Their abilities to inhibit P-glycoprotein-mediated daunorubicin efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein were evaluated versus progesterone. The hybrid with a hexamethylene linker chain showed the best inhibitory potency. The efficiency of these progesterone-adenine hybrids depends on two main factors: (i) the nature of the linker and (ii) its attachment point on the steroid skeleton.

Design, synthesis and evaluation of progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux

Steroidal bivalent ligands were designed on the basis of the described closer proximity of the ATP-site and the putative steroid-binding site of P-glycoprotein (ABCB1). The syntheses of seven progesterone-adenine hybrids were described. Their abilities to inhibit P-glycoprotein-mediated daunorubicin efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein were evaluated versus progesterone.

An oligomer-based approach to skeletal diversity in small-molecule synthesis

Access to small molecules of widely varying molecular shapes has been identified as an enabling step in the discovery of biologically active materials. In this communication we introduce an approach to the systematic development of architecturally distinc

Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery

A library of macrocyclic compounds of the formula (I) where part (A) is a (CH2)y—NH— bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a (CH2)z—NH— bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a (CH2)t—NH— bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; and where part (T) is a —Y-L-Z— radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for their preparation of these compounds in a combinatorial manner, is also disclosed.

Transmetallation from aluminum to tin: A facile preparation of tributylstannylprop-2-en-1-ols

3-Substituted 3-tributylstannylprop-2-en-1-ols 2 can be efficiently prepared by hydroalumination of 3-substituted propargyl alcohols 1 with LiAlH4 and subsequent transmetallation to tin employing Bu3SnOMe instead of the commonly used Bu3SnOTf or Bu3SnCl.