50607-30-2

Usage

Chemical Properties

White to light yellow solid

InChI:InChI=1/C5H7NO2/c7-4-1-2-6-5(8)3-4/h1-3H2,(H,6,8)

Upstream product

• 143300-67-8 Ethyl 3-[(3-ethoxy-3-oxo-propyl)amino]-3-oxo-propanoate 
• 476014-76-3 (±)-4-hydroxypiperidin-2-one 
• 1026386-87-7 ethyl 2,4-dioxopiperidine-3-carboxylate 
• 90608-67-6 1-tert-butyl-piperidine-2,4-dione 
• 845267-78-9 tert-butyl 2,4-dioxopiperidine-1-carboxylate 

Downstream Products

• 724726-05-0 2-(2-chloropyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one 
• 845714-00-3 PHA-767491 
• 128486-98-6 4-(4-fluorophenylamino)-5,6-dihydropyridin-2(1H)-one 
• 476014-76-3 (±)-4-hydroxypiperidin-2-one 
• 791-28-6 Triphenylphosphine oxide 

Relevant academic research and scientific papers

Furo-3-carboxamide derivatives and methods of use

Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, Z1, Z2, and n are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

A 2,4-piperidine dione synthetic method (by machine translation)

The invention discloses a synthetic method of 2, 4-dioxopiperidine. The method comprises the following steps: by taking monomethyl malonate, 3-amino methyl propionate hydrochloride or 3-amino ethyl propionate hydrochloride as an initial raw material, dichloromethane as a solvent, dicyclohexylcarbodiimide (DDC) as a dehydrator and triethylamine as an acid-binding agent, carrying out a reaction; acidylating a condensation product methyl-3-((3-methoxyl-3-carbonyl propyl) amino)-3-carbonyl propionate, wherein in the acidylating condensation reaction process, onium salt is used as a catalyst which is good in selectivity, few in side reaction and higher in yield; then, circularly condensing to obtain 3-(carbomethoxy(methoxycarbonyl))-4-carbonyl-1, 4, 5, 6-tetrapyridine-2-alcoholic sodium under the effect of sodium methylate; and then, decarboxylating in a hydrochloric acid system to obtain 2, 4-dioxopiperidine. In the whole reaction, as methoxyl is easy to remove, so that the synthetic method is available in the raw materials, mild in reaction condition, safe to operate and high in conversion rate.

FURO-3-CARBOXAMIDE DERIVATIVES AND METHODS OF USE

Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, Z1, Z2, and n are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

17a-HYDROXYLASE/C17,20-LYASE INHIBITORS

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.

A multifaceted secondary structure mimic based on piperidine-piperidinones

Minimalist secondary structure mimics are typically made to resemble one interface in a protein-protein interaction (PPI), and thus perturb it. We recently proposed suitable chemotypes can be matched with interface regions directly, without regard for secondary structures. Here we describe a modular synthesis of a new chemotype 1, simulation of its solution-state conformational ensemble, and correlation of that with ideal secondary structures and real interface regions in PPIs. Scaffold 1 presents amino acid side-chains that are quite separated from each other, in orientations that closely resemble ideal sheet or helical structures, similar non-ideal structures at PPI interfaces, and regions of other PPI interfaces where the mimic conformation does not resemble any secondary structure. 68 different PPIs where conformations of 1 matched well were identified. A new method is also presented to determine the relevance of a minimalist mimic crystal structure to its solution conformations. Thus dld-1-faf crystallized in a conformation that is estimated to be 0.91 kcal-mol-1 above the minimum energy solution state. Do we know, when designing a new peptidomimetic scaffold like the one shown, how it can resemble secondary structures? Design and modular synthesis of this elongated mimic is reported, and the structure is related to ideal and real structures at PPI interfaces.

Metal-free, mild, nonepimerizing, chemo- and enantio- or diastereoselective N-alkylation of amines by alcohols via oxidation/imine-iminium formation/reductive amination: A pragmatic synthesis of octahydropyrazinopyridoindoles and higher ring analogues

A mild step and atom-economical nonepimerizing chemo- and enantioselective N-alkylating procedure has been developed via oxidation/imine-iminium formation/reduction cascade using TEMPO-BAIB-HEH-Bronsted acid catalysis in DMPU as solvent and a stoichiometric amount of amine. The optimized conditions were further extended for the nonenzymatic kinetic resolution of the chiral amine thus formed under nonenzymatic in situ hydrogen-transfer conditions using VAPOL-derived phosphoric acid (VAPOL-PA) as the Bronsted acid catalyst. The enantioselective cascade of the presented reaction was successfully utilized in the synthesis of octahydropyrazinopyridoindole and its higher ring analogues.

Extending the scope of the aza-Fischer synthesis of 4- and 6-azaindoles

Fischer indole cyclization has recently been described as an efficient approach to the synthesis of azaindoles bearing electron-donating groups. We now show that this cascade reaction can be very efficient for the formation of a wider range of 4- and 6-azaindoles by using microwave irradiation. Fischer indole cyclization starting from aminopyridines is a very efficient cascade sequence leading to 4- and 6-azaindoles. The scope of the substituents on the pyridine ring was extended to include halogens and to weakly electron-donating substituents by using microwave irradiation. Copyright

17α-HYDROXYLASE/C17,20-LYASE INHIBITORS

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II

Spirocyclopropane- and spiroazetidine-substituted tetracycles 13D-E and 16A are described as orally active MK2 inhibitors. The spiroazetidine derivatives are potent MK2 inhibitors with IC50 50

INDOLONE MODULATORS OF 5-HT3 RECEPTOR

The present invention relates to new indolone modulators of 5-HT3 receptor, pharmaceutical compositions thereof, and methods of use thereof.