151978-58-4

Upstream product

• 15252-45-6 1-amino-5-hexyne 
• 24424-99-5 di-tert-butyl dicarbonate 
• 30964-00-2 hept-6-ynoic acid 
• 75-65-0 tert-butyl alcohol 
• 10297-06-0 1-chloro-5-hexyne 
• 1101108-51-3 tert-butyl N-tert-butoxycarbonyl-N-hex-5-ynyl-carbamate 
• 928-90-5 5-hexyl-1-ol 
• 51779-32-9 iminodicarboxylic acid di-tert-butyl ester 
• 6097-08-1 2-(hex-5-yn-1-yl)isoindole-1,3-dione 

Downstream Products

• 1246242-16-9 (6-cyclohex-1-enylhex-5-ynyl)carbamic acid tert-butyl ester 
• 42510-59-8 threo-8-oxa-7-phenyl-1-azabicyclo<4.3.0>nonan-9-one 
• 42510-59-8 1-phenylhexahydro-3H-oxazolo[3,4-a]pyridin-3-one 

Relevant academic research and scientific papers

Azerocyclic compounds and their uses

The present invention proposes a nitrogen heterocyclic compound and its use, in particular, the present invention proposes a new compound that effectively inhibits ATX, which is a compound shown in the formula below, or a tautomer of the compound shown be

Photocatalytic Oxyamination of Alkenes: Copper(II) Salts as Terminal Oxidants in Photoredox Catalysis

A photocatalytic method for the oxyamination of alkenes using simple nucleophilic nitrogen atom sources in place of prefunctionalized electrophilic nitrogen atom donors is reported. Copper(II) is an inexpensive, practical, and uniquely effective terminal oxidant for this process. In contrast to oxygen, peroxides, and similar oxidants commonly utilized in non-photochemical oxidative methods, the use of copper(II) as a terminal oxidant in photoredox reactions avoids the formation of reactive heteroatom-centered radical intermediates that can be incompatible with electron-rich functional groups. As a demonstration of the generality of this concept, it has been shown that diamination and deoxygenation reactions can also be accomplished using similar photooxidative conditions.

Tandem Gold-Catalyzed Dehydrative Cyclization/Diels-Alder Reactions: Facile Access to Indolocarbazole Alkaloids

A gold-catalyzed synthesis of cyclic 2-oxodienes from readily prepared propargyl alcohols and the subsequent Diels-Alder reaction are reported. The dehydrative cyclization reactions proceeded smoothly, and the dienes formed in situ were demonstrated to un

68Ga/DOTA- and 64Cu/NOTA-phthalocyanine conjugates as fluorescent/PET bimodal imaging probes

In this paper, we describe the synthesis and characterization of a series of new bimodal probes combining water-soluble sulfonated zinc phthalocyanine (ZnPc) as a fluorescence imaging unit and either 68Ga/1,4,7,10- tetraazocyclododecane-N,N′N″,N′″-tetraacetic acid (DOTA) or 64Cu/1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) for PET imaging. The two moieties were linked through aliphatic chains of different lengths to modulate amphiphilicity. Labeling of DOTA- or NOTA-ZnPc conjugates with 68Ga (t1/2 = 68 min) and 64Cu (t 1/2 = 12.7 h) was performed at 100 C for 15 min with >90% efficiency for all conjugates. In vitro plasma stability assays demonstrated high stability of the 64Cu/NOTA-ZnPc conjugate, which remained intact over a 24 h time period, and reasonably high stability of the 68Ga/DOTA-ZnPc conjugate, which released up to 7% of free 68Ga over a 3 h period. Based on in vitro plasma stability results, we performed biodistribution studies on two 64Cu-labeled derivatives, which allowed us to select a single candidate for preliminary in vivo experiments. Fluorescence and PET imaging confirmed the potential of these novel conjugates to act as bimodal probes.

Synthesis of a potent photoreactive acidic γ-secretase modulator for target identification in cells

Supramolecular self-assembly of amyloidogenic peptides is closely associated with numerous pathological conditions. For instance, Alzheimers disease (AD) is characterized by abundant amyloid plaques originating from the proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-secretases. Compounds named γ-secretase modulators (GSMs) can shift the substrate cleavage specificity of γ-secretase toward the production of non-amyloidogenic, shorter Aβ fragments. Herein, we describe the synthesis of highly potent acidic GSMs, equipped with a photoreactive diazirine moiety for photoaffinity labeling. The probes labeled the N-terminal fragment of presenilin (the catalytic subunit of γ-secretase), supporting a mode of action involving binding to γ-secretase. This fundamental step toward the elucidation of the molecular mechanism governing the GSM-induced shift in γ-secretase proteolytic specificity should pave the way for the development of improved drugs against AD.

Synthesis of a potent photoreactive acidic γ-secretase modulator for target identification in cells

Supramolecular self-assembly of amyloidogenic peptides is closely associated with numerous pathological conditions. For instance, Alzheime?s disease (AD) is characterized by abundant amyloid plaques originating from the proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-secretases. Compounds named γ-secretase modulators (GSMs) can shift the substrate cleavage specificity of γ-secretase toward the production of non-amyloidogenic, shorter Aβ fragments. Herein, we describe the synthesis of highly potent acidic GSMs, equipped with a photoreactive diazirine moiety for photoaffinity labeling. The probes labeled the N-terminal fragment of presenilin (the catalytic subunit of γ-secretase), supporting a mode of action involving binding to γ-secretase. This fundamental step toward the elucidation of the molecular mechanism governing the GSM-induced shift in γ-secretase proteolytic specificity should pave the way for the development of improved drugs against AD.

Gold-catalyzed highly regioselective oxidation of C-C triple bonds without acid additives: Propargyl moieties as masked α,β-unsaturated carbonyls

Gold-catalyzed intermolecular oxidations of internal alkynes have been achieved with high regioselectivities using 8-alkylquinoline N-oxides as oxidants and in the absence of acid additives. Synthetically versatile α,β-unsaturated carbonyls are obtained in good to excellent yields and with excellent E-selectivities. A range of functional groups such as THP, MOMO, N3, OTBS, and N-Boc are tolerated. This reaction allows α,β-unsaturated carbonyls to be masked as propargyl moieties, thus offering a practical solution to compatibility issues with these functional groups likely encountered in syntheses of complex structures.

Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III receptor

A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPIIb IIIa receptor and is provided in therapeutic compositions for t