57477-12-0

Usage

InChI:InChI=1/C13H17NO4/c1-3-17-12(15)11(13(16)18-4-2)8-10-6-5-7-14-9-10/h5-7,9,11H,3-4,8H2,1-2H3

Upstream product

• 53361-09-4 diethyl 2-((pyridin-3-yl)methylene)malonate 
• 3099-31-8 nicotinyl chloride 
• 105-53-3 diethyl malonate 
• 500-22-1 3-pyridinecarboxaldehyde 
• 996-82-7 sodium diethylmalonate 
• 6959-48-4 3-chloromethylpyridinium chloride 

Downstream Products

• 1345343-82-9 C₁₉H₂₅N₃O₄ 
• 1345343-98-7 (E)-cyclo[N-cyclohexyloxy-2-[(β-pyridyl)methylene]glycylprolyl] 
• 1345343-72-7 ethyl 2-cyclohexyloxyimine-3-b-pyridylpropionate 
• 134208-94-9 7,7-bis(ethoxycarbonyl)-5-phenyl-7,8-dihydroisoquinoline 
• 134208-93-8 6,6-bis(ethoxycarbonyl)-8-phenyl-5,6-dihydroquinoline 
• 134208-82-5 6,6-bis(ethoxycarbonyl)-8-phenyl-5,6,7,8-tetrahydroquinoline 
• 134208-83-6 5-phenyl-7,7-bis(ethoxycarbonyl)-5,6,7,8-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines

A series of arylidene N-alkoxydiketopiperazines was designed and stereoselectively synthesized via oxime-ether formation and intramolecular acylation. Possible cyclization and acid-catalyzed rearrangement-fragmentation mechanisms were discussed. The crystal structure of the novel diketopiperazine further confirmed the rearrangement mechanism. Most compounds exhibited antitumor activity. Several compounds were more potent against caspase-3. Specifically, compounds 6e, 6g, and 6f inhibited caspase-3 at IC50values lying within the low micromolar range and demonstrated good selectivity. The binding modes of alkoxydiketopiperazines in the active center of caspase-3 were also discussed based on the molecular docking results.

BETA-MERCAPTO-PROPANAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISEASES

Compounds of formula STR1 wherein R, R 1, R 2, Het and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.

Beta-mercapto-propanamide derivatives useful in the treatment of cardiovascular diseases

Compounds of formula wherein R, R1, R2, Het and nhave the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.

A novel class of enkephalinase inhibitors containing a C-terminal sulfo group

A new series of sulfonic acids were synthesized and tested for their enkephalinase inhibitory activity. Among them, the most potent was N-(2- benzyl-3-mercaptopropionyl)metanilic acid 10i with an IC50 value of 0.27 nM. Several other analogues (10a,b,j,n,o,gg,hh) showed the inhibitory activity comparable to or greater than thiorphan (IC50 = 2.6 nM), a C- terminal carboxyl-containing inhibitor of enkephalinase. Thus compounds containing a C-terminal sulfo group, instead of the C-terminal carboxyl group, were found to show a remarkably high level of inhibition of enkephalinase. The analgesic activity of 10b, (S)-10b, and (R)-10b was also evaluated by the phenylbenzoquinone writhing test.

Oxidation of Diethyl (Pyridylmethyl)malonates with Mn(III) Acetate, Ce(IV) Ammonium Nitrate, and Iron(III) Perchlorate in the Presence of Alkenes and Alkynes

The oxidation of substituted diethyl 2-,3-, or 4-picolylmalonates (1a-g) by Mn(III) acetate in acetic acid, Ce(IV) ammonium nitrate in methanol, and Fe(III) perchlorate in acetonitrile in the presence of substituted alkenes (2) and alkynes (3) affords substituted tetra- or dihydroquinolines and/or isoquinolines (4-9) in good to excellent yield.The influence of reaction medium on yield and isomer distribution has been investigated.A mechanism involving oxidative deprotonation of malonic esters by high-valent metal salts to malonyl radicals, their addition to olefins, and intramolecular homolytic substitution to protonated or metal-complexed heteroaromatic bases by the resulting substituted carbon radicals is suggested.