177947-96-5

Usage

Uses

Used in Pharmaceutical Industry:
3-FORMYL-AZETIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is used as an intermediate for the development of various pharmaceuticals. Its unique structure allows for the creation of novel drug candidates with potential therapeutic applications.
Used in Organic Synthesis:
3-FORMYL-AZETIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a starting material in organic synthesis. Its versatile chemical structure enables the synthesis of a wide range of organic compounds, including those with potential applications in various industries such as agriculture, materials science, and chemical manufacturing.

Upstream product

• 201230-82-2 carbon monoxide 
• 1248510-38-4 tert-butyl azete-1(2H)-carboxylate 
• 398489-26-4 tert-butyl 3-oxoazetidine-1-carboxylate 
• 4009-98-7 (methoxymethyl)triphenylphosphonium chloride 
• 142253-56-3 3-hydroxymethyl-azetidine-1-carboxylic acid tert-butyl ester 
• 142253-54-1 tert-butyl 3-cyanoazetidine-1-carboxylate 
• 610791-05-4 azetidine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester 
• 142253-55-2 1-(t-butyloxycarbonyl)-azetidine-3-carboxylic acid 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 193085-21-1 3-((E)-2-ethoxycarbonylvinyl)azetidine-1-carboxylic acid tert-butyl ester 
• 193085-22-2 3-((E)-2-carboxyvinyl)azetidine-1-carboxylic acid tert-butyl ester 
• 193085-23-3 3-((E)-2-(methyl((1R)-1-(methyl((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)carbamoyl)vinyl)azetidine-1-carboxylic acid tert-butyl ester 
• 875004-86-7 3-[4-(3-acetylaminophenyl)piperidin-1-ylmethyl]azetidine-1-carboxylic acid tert-butyl ester 
• 887590-28-5 C₁₄H₂₁N₃O₂ 
• 1108746-93-5 tert-butyl 3-{[(4-{[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]carbamoyl}-3-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]phenyl)amino]methyl}azetidine-1-carboxylate 
• 1105070-81-2 3-{(hydroxy)[2-(methylsulphanyl)thieno[2,3-b]pyridin-3-yl]methyl}azetidine-1-carboxylic acid tert-butyl ester 
• 1197419-14-9 C₁₀H₁₅Br₂NO₂ 
• 1228230-94-1 3-[hydroxy-(4-methoxy-phenyl)-methyl]-azetidine-1-carboxylic acid tert-butyl ester 
• 1228230-88-3 3-(hydroxy-pyridin-2-yl-methyl)-azetidine-1-carboxylic acid tert-butyl ester 
• 1234710-02-1 tert-butyl 3-(1H-imidazol-2-yl)azetidine-1-carboxylate 
• 1296689-98-9 C₁₃H₂₂N₂O₃ 
• 1296689-87-6 C₂₆H₃₄N₂O₄ 
• 1215121-77-9 TERT-BUTYL 3-[(1E)-3-OXOPROP-1-ENYL]AZETIDINE-1-CARBOXYLATE 

Relevant academic research and scientific papers

CDK9 Kinase inhibitors

The present application relates to CDK9 kinase inhibitors which provide a compound of formula (I) or a stereoisomer thereof. A solvate, a metabolite, a pharmaceutically acceptable salt or prodrug, and a pharmaceutical composition comprising the same. Also provided are the use of compounds and pharmaceutical compositions in the manufacture of a medicament for the treatment of cancer.

X-ray Structure-Guided Discovery of a Potent, Orally Bioavailable, Dual Human Indoleamine/Tryptophan 2,3-Dioxygenase (hIDO/hTDO) Inhibitor That Shows Activity in a Mouse Model of Parkinson’s Disease

Human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) have been closely linked to the pathogenesis of Parkinson’s disease (PD); nevertheless, development of dual hIDO1 and hTDO inhibitors to evaluate their potential efficacy against PD is still lacking. Here, we report biochemical, biophysical, and computational analyses revealing that 1H-indazole-4-amines inhibit both hIDO1 and hTDO by a mechanism involving direct coordination with the heme ferrous and ferric states. Crystal structure-guided optimization led to23, which manifested IC50values of 0.64 and 0.04 μM to hIDO1 and hTDO, respectively, and had good pharmacokinetic properties and brain penetration in mice.23showed efficacy against the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse motor coordination deficits, comparable to Madopar, an anti-PD medicine. Further studies revealed that different from Madopar,23likely has specific anti-PD mechanisms involving lowering IDO1 expression, alleviating dopaminergic neurodegeneration, reducing inflammatory cytokines and quinolinic acid in mouse brain, and increasing kynurenic acid in mouse blood.

?-LACTAMASE INHIBITOR AND USE THEREOF

Provided are a β-lactamase inhibitor of formula (I), or an ester, a stereoisomer or a pharmaceutically acceptable salt thereof, and a method of preparing the same. Further provided is a pharmaceutical composition comprising the β-lactamase inhibitor of formula (I), or the ester, the stereoisomer or pharmaceutically acceptable salt thereof. In addition, the present invention relates to a method for treating diseases caused by bacterial infection, which comprises administering the β-lactamase inhibitor of formula (I), or the ester, the stereoisomer or the pharmaceutically acceptable salt thereof to a patient or a subject in need.

Facile synthesis of 2-azaspiro[3.4]octane

Our annulation strategy utilized for the synthesis of 2-azaspiro[3.4]octane is explained. Three successful routes for the synthesis were developed. One of the approaches involved annulation of the cyclopentane ring and the remaining two approaches involved annulation of the four membered ring. All three approaches employ readily available starting materials with conventional chemical transformations and minimal chromatographic purifications to afford the title compound. The merits and limitations of the three approaches are also discussed.

TARGETING COMPOUNDS

The disclosure provides, at least in part, liver, intestine and/or kidney-targeting compounds and their use in treating liver, intestine and/or kidney disorders, such as non-alcoholic steatohepatitis, alcoholic steatohepatitis, hepatocellular carcinoma, liver cirrhosis, and hepatitis B; and/or chronic kidney disease, glomerular disease such as IGA nephropathy, lupus nephritis, or polycystic kidney disease. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

MCL-1 INHIBITORS

The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.

Production methods of nitrogen heterocyclic carboxylic acid intermediate and 3-azetidine carboxylic acid

The invention discloses production methods of a nitrogen heterocyclic carboxylic acid intermediate and 3-azetidine carboxylic acid, and relates to the technical field of pharmaceutical and chemical industry. The production method of the nitrogen heterocyclic carboxylic acid intermediate used for producing the 3-azetidine carboxylic acid comprises the steps of mixing a nitrogen heterocyclic compound and a Wittig reaction agent, carrying out a Wittig reaction, and conducting separation to obtain a nitrogen heterocyclic formaldehyde intermediate; and subjecting the nitrogen heterocyclic formaldehyde intermediate to an oxidation reaction, and conducting separation to obtain the nitrogen heterocyclic carboxylic acid intermediate, wherein the nitrogen heterocyclic compound is selected from at least one of 1-benzhydrylazetidin-3-one, 1-benzylazetidin-3-one, 1-Boc-3-azetidinone and 1-acetylazetidin-3-one. According to the production method of the 3-azetidine carboxylic acid, the nitrogen heterocyclic carboxylic acid intermediate is subjected to hydrogenolysis, a production cycle is short, a production process is safe and reliable, the production cost is low, the purity is higher than 98%,and the yield can reach 82.8%.

CYCLOBUTANE- AND AZETIDINE-CONTAINING MONO AND SPIROCYCLIC COMPOUNDS AS ALPHA V INTEGRIN INHIBITORS

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αv- containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

AZOLE-SUBSTITUTED PYRIDINE COMPOUND

The present invention provides a compound represented by formula [I'| shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme, wherein the structure represented by formula [III] shown below represents any of the structures represented by formula group [IV] shown below, wherein R1 represents a hydrogen atom, a fluorine atom, methyl, etc.; R2, R3, and R4 each independently represent a hydrogen atom, a fluorine atom, or methyl; W represents a single bond, C1-3alkanediyl, or the formula -O-CH2CH2-; and ring A represents (a) substituted C4-6cycloalkyl, (b) substituted 4- to 6-membered saturated nitrogen-containing heterocyclyl, (c) substituted phenyl, (d) substituted pyridyl, (e) substituted 2,3-dihydrobenzofuran, (f) 4- to 6-membered saturated oxygen-containing heterocyclyl, etc.

Polysubstituted-indazole compounds and application of same as IDO inhibitors

The invention discloses polysubstituted-indazole compounds as shown in a formula (I) which is described in the specification, a preparation method for the compounds, and application of the compounds as IDO inhibitors. The compounds provided by the invention can be used for preventing and/or treating a plurality of diseases, such as Alzheimer's disease, cataract, infections related to cellular immune activation, autoimmune diseases, AIDS, cancers, depression, the metabolic disorder of tryptophan or the like.