479630-08-5

Usage

Uses

Used in Pharmaceutical Industry:
4-(2-Ethoxycarbonyl-acetyl)-piperidine-1-carboxylic acid tert-butyl ester is used as a building block or intermediate for the synthesis of various pharmaceutical compounds. Its presence in the piperidine family allows for the creation of a wide range of drug molecules with potential therapeutic applications.
Used in Agrochemical Industry:
4-(2-Ethoxycarbonyl-acetyl)-piperidine-1-carboxylic acid tert-butyl ester is used as a precursor in the development of agrochemicals, such as pesticides and herbicides. Its chemical structure can be modified to create compounds with specific pesticidal or herbicidal properties.
Used in Materials Science:
4-(2-Ethoxycarbonyl-acetyl)-piperidine-1-carboxylic acid tert-butyl ester is used as a component in the synthesis of advanced materials, such as polymers and coatings, that can be tailored for specific applications. Its versatility in chemical reactions enables the creation of materials with unique properties.

InChI:InChI=1/C15H25NO5/c1-5-20-13(18)10-12(17)11-6-8-16(9-7-11)14(19)21-15(2,3)4/h11H,5-10H2,1-4H3

Upstream product

• 498-94-2 isonipecotic acid 
• 64-17-5 ethanol 
• 1336874-02-2 tert‐butyl 4‐(2,2‐dimethyl‐4,6‐dioxo‐1,3‐dioxane‐5‐carbonyl)piperidine‐1‐carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 
• 6148-64-7 ethyl potassium malonate 
• 293744-38-4 tert-butyl 4-(1H-imindazole-1-carbonyl)piperidine-1-carboxylate 
• 91419-52-2 1-tert-butoxycarbonyl-4-cyanopiperidine 
• 105-36-2 ethyl bromoacetate 
• 124443-68-1 1-tert-Butyl 4-methyl piperidine-1,4-dicarboxylate 
• 782493-40-7 tert-butyl 4-[(2,2-dimethyl-4,6-dioxo-1,3-dioxan-5-ylidene)(hydroxy)methyl]piperidine-1-carboxylate 
• 38330-80-2 monomethyl monopotassium malonate 
• 141-78-6 ethyl acetate 
• 142851-03-4 1-tert-butyl 4-ethyl piperidine-1,4-dicarboxylate 

Downstream Products

• 1020196-55-7 N-(3,5-dimethylphenyl)-1-(4-isopropylphenyl)-5-(piperidin-4-yl)-1H-pyrazole-4-carboxamide 
• 957247-54-0 tert-butyl 4-(4-(ethoxycarbonyl)-1-(4-isopropylphenyl)-1H-pyrazol-5-yl)piperidine-1-carboxylate 
• 1020050-02-5 5-(1-(tert-butoxycarbonyl)piperidin-4-yl)-1-(4-isopropylphenyl)-1H-pyrazole-4-carboxylic acid 
• 1020050-10-5 tert-butyl 4-(4-((3,5-dimethylphenyl)carbamoyl)-1-(4-isopropylphenyl)-1H-pyrazol-5-yl)piperidine-1-carboxylate 
• 1373491-61-2 6-(1-(3-hydroxy-4-methoxybenzyl)piperidin-4-yl)-2-piperidin-1-ylpyrimidin-4-ol 

Relevant academic research and scientific papers

Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia

Parthenolide is a natural product that exhibits anti-leukaemic activity, however, its clinical use is limited by its poor bioavailability. It may be extracted from feverfew and protocols for growing, extracting and derivatising it are reported. A novel parthenolide derivative with good bioavailability and pharmacological properties was identified through a screening cascade based on in vitro anti-leukaemic activity and calculated "drug-likeness" properties, in vitro and in vivo pharmacokinetics studies and hERG liability testing. In vitro studies showed the most promising derivative to have comparable anti-leukaemic activity to DMAPT, a previously described parthenolide derivative. The newly identified compound was shown to have pro-oxidant activity and in silico molecular docking studies indicate a prodrug mode of action. A synthesis scheme is presented for the production of amine 7 used in the generation of 5f.

DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES

The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.

Reformatsky and Blaise reactions in flow as a tool for drug discovery. One pot diversity oriented synthesis of valuable intermediates and heterocycles

The application of Reformatsky and Blaise reactions for the preparation of a diverse set of valuable intermediates and heterocycles in a one-pot protocol is described. To achieve this goal, a greener activation protocol for zinc in flow conditions has been developed to introduce this metal efficiently into α-bromoacetates. The organozinc compounds were added to a diverse set of ketones and nitriles to obtain a wide range of functional groups and heterocyclic systems.

Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels

Transient receptor potential canonical 3/6/7 (TRPC3/6/7) are highly homologous receptor-operated nonselective cation channels. Despite their physiological significance, very few selective and potent agonists are available for functional examination of these channels. Using a cell-based high throughput screening approach, a lead compound with the pyrazolopyrimidine skeleton was identified as a TRPC6 agonist. Synthetic schemes for the lead and its analogues were established, and structural-activity relationship studies were carried out. A series of potent and direct agonists of TRPC3/6/7 channels were identified, and among them, 4m-4p have a potency order of TRPC3 > C7 > C6, with 4n being the most potent with an EC50 of 20 nM on TRPC3. Importantly, these compounds exhibited no stimulatory activity on related TRP channels. The potent and selective compounds described here should be suitable for evaluation of the roles of TRPC channels in the physiology and pathogenesis of diseases, including glomerulosclerosis and cancer.

Compounds and methods for treating cancer by inhibiting the urokinase receptor

Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.

FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.

Benzonaphthyrindines compounds and pharmaceutical compositions thereof and its application in pharmacy

The invention provides a pyrazolopyrimidine compound shown as a structural formula (I), a pharmaceutical composition taking the pyrazolopyrimidine compound as an active component, a preparation method of the pyrazolopyrimidine compound and the pharmaceutical composition as well as an application of the pyrazolopyrimidine compound and the pharmaceutical composition in preparation of a TRPC6 (Transient Receptor Potential Channel 6) adjustor probe medicine and related medicines for preventing and treating glomerulopathy and myocardial hypertrophy. The pyrazolopyrimidine compound and derivatives provided by the invention can be used to prepare medical preparations in various forms which comprise oral liquids, injections, pulmonary inhalation preparations and transdermal preparations, specifically injections, oral liquids, troches, capsules, granules, aerosols, dry powder inhalation, patches and the like.

PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVE AND USE OF ANTI-TUMOR THEREOF

The present invention relates to a pyrazolo[1,5-a]pyrimidine derivative of general formula 1 and a pharmaceutically acceptable salt thereof. The present invention also relates to use of compounds of formula 1 in the preparation of an anti-tumor medicament.

PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

(Aza)pyridopyrazolopyrimidinones and indazolopyrimidinones and their use

The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.