133010-02-3

Upstream product

• 13734-41-3 N-Boc-(S/R)-valine 
• 675-14-9 trifluoro-[1,3,5]triazine 
• 13734-41-3 t-Boc-L-valine 

Downstream Products

• 87694-52-8 tert-butyl (S)-1-(N-methoxy-N-methylcarbamoyl)-2-methylpropylcarbamate 
• 1400436-05-6 C₄₀H₆₇N₅O₁₀ 
• 1400437-15-1 C₃₁H₅₂N₄O₇*C₂HF₃O₂ 
• 1400437-11-7 C₃₁H₅₂N₄O₇*C₂HF₃O₂ 
• 1400437-33-3 C₄₅H₇₂N₆O₁₀S 
• 1427500-60-4 C₄₁H₆₆N₆O₈S 
• 1427500-59-1 C₄₀H₆₄N₆O₈S 

Relevant academic research and scientific papers

Rapid and column-free syntheses of acyl fluorides and peptides usingex situgenerated thionyl fluoride

Thionyl fluoride (SOF2) was first isolated in 1896, but there have been less than 10 subsequent reports of its use as a reagent for organic synthesis. This is partly due to a lack of facile, lab-scale methods for its generation. Herein we report a novel protocol for theex situgeneration of SOF2and subsequent demonstration of its ability to access both aliphatic and aromatic acyl fluorides in 55-98% isolated yields under mild conditions and short reaction times. We further demonstrate its aptitude in amino acid couplings, with a one-pot, column-free strategy that affords the corresponding dipeptides in 65-97% isolated yields with minimal to no epimerization. The broad scope allows for a wide range of protecting groups and both natural and unnatural amino acids. Finally, we demonstrated that this new method can be used in sequential liquid phase peptide synthesis (LPPS) to afford tri-, tetra-, penta-, and decapeptides in 14-88% yields without the need for column chromatography. We also demonstrated that this new method is amenable to solid phase peptide synthesis (SPPS), affording di- and pentapeptides in 80-98% yields.

HETEROAROMATIC DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF

Provided herein are novel heteroaromatic derivatives, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a prodrug, a pharmaceutically acceptable salt or a prodrug thereof, and pharmaceutical compositions containing such compounds. Also provided herein are uses of such compounds or pharmaceutical compositions thereof in the manufacture of a medicament for treating respiratory diseases, especially chronic obstructive pulmonary disease (COPD).

Oligopeptides and process for preparation thereof

This invention relates to oligopeptides having general formula (I). The invention also relates to the process of preparation thereof, wherein the said compounds are selective anti-cancer agents over a panel of human cancer cell lines. Further, this invent

A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death

We have synthesized eight analogues (D1-D8) of dolastatin 10 containing several unique amino acid subunits. Of these agents, D5 was found to be most effective in inhibiting both HeLa cell proliferation and microtubule assembly in vitro. At low nanomolar concentrations, D5 inhibited the proliferation of several types of cancer cells in culture. D5 bound to tubulin with a dissociation constant of 29.4 ± 6 μM. D5 depolymerized microtubules in cultured cells and produced mulitpolar spindles. At its half-maximal inhibitory concentration (15 nM), D5 strongly suppressed the dynamics of individual microtubules in live MCF-7 cells. D5 increased the accumulation of checkpoint proteins BubR1 and Mad2 at the kinetochoric region and caused G2/M block in these cells. The blocked cells underwent apoptosis with the activation of Jun N-terminal kinase. The results suggested that D5 exerts its antiproliferative action by dampening microtubule dynamics.

A supramolecular approach to chiral ligand modification: Coordination chemistry of a multifunctionalised tridentate amine-phosphine ligand

A novel chiral amine-phosphine tagged with an amido-napthyridine moiety has been synthesised and found to bind complementary pyridinone additives. These additives were found to have a modest but measurable promotional effect on the catalytic activity and/or enantioselectivity of Ir- and Rh-catalysed reductions. One explanation for the relatively poor results obtained with the Ir and Ru catalysts is the formation of complexes, in which the ligand adopts an anionic tridentate coordination mode. Pt and Rh complexes of this type were isolated and characterised. The Royal Society of Chemistry and the Centre National de la Recherche Scientifique.

Self-assembly of organocatalysts: Fine-tuning organocatalytic reactions

(Chemical Equation Presented) A cat. with two tales: Hydrogen-bonding interactions between achiral pyridinone additives and unselective chiral proline-derived organocatalysts (see picture) result in highly effective catalysts for the Michael addition of n

Effects of steric bulk and stereochemistry on the rates of?diketopiperazine formation from N-aminoacyl-2,2-dimethylthiazolidine-4-carboxamides (Dmt dipeptide amides)-a model for a new prodrug linker system

A peptide-like self-immolative molecular clip is required for release of active drugs from prodrugs by endopeptidases. Upon cleavage from the carrier, this clip must collapse and release the drug rapidly. A series of aminoacyl-5,5-dimethylthiaproline (Aaa

SUBSTITUTED 2-AMINO- 1,2,4 TRIAZOLO 1,5-a PYRIMIDINE DERIVATIVE AND USE THEREOF

Disclosed is a [1,2,4]triazolo[1,5-a]pyrimidine derivative represented by the general formula (I) below or a pharmaceutically acceptable salt thereof. Also disclosed is a medicine containing such a derivative or a salt thereof as an active constituent. In

[Bis(2-methoxyethyl)amino]sulfur Trifluoride, the Deoxo-Fluor Reagent: Application toward One-Flask Transformations of Carboxylic Acids to Amides

The use of the Deoxo-Fluor reagent is a versatile method for acyl fluoride generation and subsequent one-flask amide coupling. It provides mild conditions and facile purification of the desired products in good to excellent yields. We have explored the utility of this reagent for the one-flask conversion of acids to amides and Weinreb amides and as a peptide-coupling reagent.

Development of orally active nonpeptidic inhibitors of human neutrophil elastase

5-Amino-2-phenylpyrimidin-6-ones, some of their desamino derivatives, and miscellaneous derivatives were synthesized and biologically evaluated on both in vitro activity and oral activity in an acute hemorrhagic assay. These compounds contained an α-keto-1,3,4-oxadiazole moiety to bind covalently to the Ser-195 hydroxy group of human neutrophil elastase (HNE). Among those tested, compounds 11a-c,e,i-l(F), 11d,e,k(H), 21d,e,k(F), and 21d,e(H) showed a good oral profile. RS-Mixture 3(H) was selected for clinical evaluation based on its oral potency, duration of action, enzyme selectivity, safety profile, and ease of synthesis. Structure -activity relationships (SARs) are discussed.