68074-14-6

Upstream product

• 201230-82-2 carbon monoxide 
• 15252-44-5 1-amino-pent-4-yne 
• 76220-94-5 3-(hydroxymethyl)-2-pyrrolidinone 
• 25219-43-6 3-(hydroxymethyl)-2-piperidinone 
• 5558-11-2 5-aminopenta-1,2-diene 
• 3731-16-6 3-carboethoxy-2-pyridone 
• 36821-26-8 2-oxopyrrolidine-3-carboxylic acid ethyl ester 
• 930608-65-4 HC₂C₃H₆NHCH(CH₃)C₆H₅ 
• 688-73-3 tri-n-butyl-tin hydride 
• 1035042-29-5 (2-oxo-3-piperidinyl)methyl methanesulfonate 
• 5390-04-5 pent-1-yn-5-ol 

Downstream Products

• 76221-10-8 3-methylene-2-oxo-α-phenyl-1-piperidineacetic acid 
• 343234-94-6 3-<(acetylthio)methyl>-2-oxo-α-phenyl-1-piperidineacetic acid 
• 68074-17-9 2-acetylthiomethyl-5-(p-methoxybenzyloxycarbonyl)aminopentanoic acid 
• 68074-16-8 2-Methylene-5-(p-methoxybenzyloxycarbonyl)aminopentanoic acid 
• 440677-00-9 3-methylene-2-oxo-piperidine-1-carboxylic acid benzyl ester 
• 870290-79-2 (6S,7S)-9-(tert-Butyl-dimethyl-silanyloxy)-8-methyl-1-oxo-7-prop-1-ynyl-2-aza-spiro[5.5]undec-8-ene-2-carboxylic acid benzyl ester 
• 1346437-29-3 C₂₂H₂₄F₃NO₆S₂ 
• 1346437-28-2 C₂₁H₂₅NO₄S 

Relevant academic research and scientific papers

Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation

Selective clearance of senescent cells (SCs) has emerged as a potential therapeutic approach for age-related diseases, as well as chemotherapy- and radiotherapy-induced adverse effects. Through a cell-based phenotypic screening approach, we recently identified piperlongumine (PL), a dietary natural product, as a novel senolytic agent, referring to small molecules that can selectively kill SCs over normal or non-senescent cells. In an effort to establish the structure-senolytic activity relationships of PL analogues, we performed a series of structural modifications on the trimethoxyphenyl and the α,β-unsaturated δ-valerolactam rings of PL. We show that modifications on the trimethoxyphenyl ring are well tolerated, while the Michael acceptor on the lactam ring is critical for the senolytic activity. Replacing the endocyclic C2–C3 olefin with an exocyclic methylene at C2 render PL analogues 47–49 with increased senolytic activity. These α-methylene containing analogues are also more potent than PL in inducing ROS production in WI-38 SCs. Similar to PL, 47–49 reduce the protein levels of oxidation resistance 1 (OXR1), an important oxidative stress response protein that regulates the expression of a variety of antioxidant enzymes, in cells. This study represents a useful starting point toward the discovery of senolytic agents for therapeutic uses.

COMPOSITIONS AND METHODS FOR SELECTIVELY DEPLETING SENESCENT CELLS

The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises piperlongumine (PL) or derivative thereof. The selective killing of senescent cells may delay aging and/or treat age-related disorders.

HERBICIDAL COMPOUNDS

The invention relates to haloalkylsulphonamide derivatives of the formula (I) wherein A, W, X, m, n, p, R, R1, R2, R5, R6, R7 and R8 are as defined in the specification. Furthermore, the present invention relates to processes for making compounds of formula (I), to herbicidal compositions comprising these compounds and to methods of using these compounds to control or inhibit plant growth.

Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4)

Structure-activity relationship studies of the cyclopentapeptide CXCR4 antagonists (cyclo(-l-/d-Arg1-Arg2-2-Nal 3-Gly4-d-Tyr5-)) suggest that the l-/d-Arg 1-Arg2-2-Nal3/sup

Radical carbonylation of ω-alkynylamines leading to α-methylene lactams. Synthetic scope and the mechanistic insights

Tin hydride mediated radical carbonylation and cyclization reaction was investigated using a variety of ω-alkynyl amines as substrates. In this reaction α-methylene and α-stannylmethylene lactams having five to eight membered rings were obtained as princi

4-BENZYL-1(2H)-PHTHALAZINONES AS H1 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula (I) and salts thereof, process for preparation thereof, to compositions containing the same and to the use of such a compound in the treatment of various diseases, such as allergic rhinitis.

Novel spiroheterocycles by aziridination of α-methylene-γ- and -δ-lactams

New potentially bioactive α-spiroaziridino-γ- and -δ-lactams have been prepared by treatment of α-methylene-γ- and -δ-lactams with ethyl N-([(4-nitrophenyl)sulfonyl]oxy)-carbamate (NsONHCO2Et) in the presence of CaO. These compounds, through reductive aziridine ring opening, can be intermediates for the synthesis of α- and β-aminolactams, which are useful as conformational constraints in peptides. The above procedure has been successfully extended to one α-methyleneoxindole to obtain a new spirooxindole derivative, a potential precursor of natural alkaloids. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.

Ruthenium-Catalyzed Cyclocarbonylation of Allenyl Alcohols and Amines: Selective Synthesis of Lactones and Lactams

Allenyl alcohols such as 4-hydroxybuta-1,2-dienes and 5-hydroxypenta-1,2-dienes having a variety of substituents undergo cyclocarbonylation in the presence of a ruthenium catalyst under mild conditions selectively to give five- and six-membered lactones in a high yield with 100% atom economy. 5-Aminopenta-1,2-dines are also cyclocarbonylated to give γ-lactams. A possible carbonylation mechanism involving a ruthenium cluster intermediate is proposed on the basis of experimental results.

Studies toward (-)-Gymnodimine: concise routes to the spirocyclic and tetrahydrofuran moieties

(formula presented) (-)-Gymnodimine is a member of a unique class of potent marine toxins possessing imines within a spirocylic array. Herein we report the synthesis of the tetrahydrofuran fragment and a strategy toward the spirocyclic imine fragment of this family of toxins. Key reactions include an asymmetric anti-aldol reaction to set the stereochemistry of the tetrahydrofuran and a formal, intermolecular Diels-Alder reaction involving an α-methylene-δ-lactam and a dienyne.

Indole derivatives as 5HT1 -like agonists

Compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates (including hydrates) of either entity, wherein R1 is (a) R2 is R3 R4 C(OH)A; V is C=O or CH2/su