915976-32-8

Basic information

• Product Name: (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate
• Synonyms: (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate;1-tert-Butyl 2-methyl (2S,5S)-5-hydroxypiperidine-1,2-dicarboxylate;(2S,5S)-5-Hydroxy-1,2-piperidinedicarboxylic acid 1-(1,1-dimethylethyl) 2-methyl ester
• CAS NO: 915976-32-8
• Molecular Formula: C₁₂H₂₁NO₅
• Molecular Weight: 259.29884
• Mol File: 915976-32-8.mol

Chemical Properties

• Appearance: /
• Storage Temp.: 2-8°C
• CAS DataBase Reference: (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate(915976-32-8)
• EPA Substance Registry System: (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate(915976-32-8)

Safety Data

• Hazardous Substances Data: 915976-32-8(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Research and Development:
(2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate is used as a key intermediate in the synthesis of various drugs and drug candidates. Its unique structural features, including the tert-butyl and methyl groups, as well as the hydroxyl group, make it a versatile building block for the development of new pharmaceutical agents.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate is employed as a chiral synthon for the asymmetric synthesis of biologically active compounds. Its stereochemistry and functional groups can be further modified to create novel molecules with potential therapeutic applications.
Used in Drug Design:
(2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate is utilized in drug design to explore its potential as a lead compound for the treatment of various diseases. Its unique structure and functional groups can be optimized to enhance its pharmacological properties, such as potency, selectivity, and bioavailability.
Used in Drug Synthesis:
In the synthesis of drugs, (2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate serves as a valuable precursor for the preparation of various pharmaceutical agents. Its reactivity and compatibility with different synthetic routes make it an attractive candidate for the development of new drug molecules.
Used in Drug Discovery:
(2S,5S)-1-tert-butyl 2-Methyl 5-hydroxypiperidine-1,2-dicarboxylate is employed in drug discovery as a starting material for the generation of compound libraries. Its structural diversity and synthetic accessibility make it an ideal candidate for high-throughput screening and the identification of novel bioactive molecules.

Upstream product

• 124-41-4 sodium methylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 67-56-1 methanol 
• 1487347-86-3 (2S,5S)-N-tert-butoxycarbonyl-5-hydroxy-2-carboxylic acid piperidine 
• 63088-78-8 (2S,5R)-5-hydroxypiperidine-2-carboxylic acid 
• 695183-75-6 (2S,5S)-5-hydroxypiperidin-2-carboxylic acid methyl ester 
• 108963-96-8 (S)-1-tert-butoxycarbonyl-5-methoxycarbonyl-pyrrolidin-2-one 
• 915976-31-7 1-(tert-butyl) 2-methyl (S)-5-oxopiperidine-1,2-dicarboxylate 

Downstream Products

• 1463501-48-5 (2S,5R)-6-(benzyloxy)-2-(hydroxymethyl)-1,6-diazabicyclo[3.2.1]octan-7-one 
• 1416134-73-0 (2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxylate methyl ester 
• 915976-31-7 1-(tert-butyl) 2-methyl (S)-5-oxopiperidine-1,2-dicarboxylate 

Relevant articles and documents

METHOD FOR PRODUCING AMINO ACID DERIVATIVES

The present invention aims to provide a method for producing a (2S,5R)-5-(protected oxyamino)-piperidine-2-carboxylic acid derivative at a low cost that can be performed under mild reaction conditions not requiring a facility at an extremely low temperature, is safer, can control the quality of the desired product with ease, and shows good workability in the site of production. A method for producing a compound represented by the formula (2): wherein PG1 is an amino-protecting group, PG2 is an amino-protecting group, PG3 is a hydroxyl-protecting group, LG is a leaving group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s), including a step of reacting a compound represented by the formula (1): wherein each symbol is as defined above, with a hydroxylamine derivative represented by the formula PG2NHOPG3 wherein each symbol is as defined above, in the presence of a base in a solvent.

Five-membered heteroaromatic derivative, preparation method and application thereof

The invention belongs to the technical field of medicines, and particularly relates to a five-membered heteroaromatic compound, a composition, a preparation method and application thereof. The compound or the composition can be used as an inhibitor of a retinoid-related orphan receptor [gamma]t (ROR [gamma]t). The invention also relates to a method for preparing the compound and the composition, and application of the compound and the composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.

ROR [gamma]t inhibitor, preparation method and application thereof

The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.

RORγ ANTAGONIST AND APPLICATION THEREOF IN MEDICINE

Provided herein are compounds as RORγ antagonist having Formula (I). The compounds or pharmaceutical composition thereof can be used for regulating Retinoid-related orphan receptor gamma t (RORγt). Also provided herein are methods of preparation of the compounds and composition thereof, and uses thereof in treating or preventing RORγt mediated inflammation or autoimmune diseases in mammals, particularly humans.

NEW BETA-LACTAMASE INHIBITORS TARGETING GRAM NEGATIVE BACTERIA

The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as β-lactamase inhibitors, notably in the treatment of a disease caused by gram negative bacteria, in particular enterobacteria, as well as pharmaceutical compositions containing such a compound and a process to prepare such a compound.

NEW ANTIBIOTICS TARGETING MYCOBACTERIA

The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as a drug, notably in the treatment of a disease caused by mycobacteria, as well as pharmaceutical compositions containing such a compound and a process to prepare such a compound.

Synthesis of Avibactam Derivatives and Activity on β-Lactamases and Peptidoglycan Biosynthesis Enzymes of Mycobacteria

There is a renewed interest for β-lactams for treating infections due to Mycobacterium tuberculosis and M. abscessus because their β-lactamases are inhibited by classical (clavulanate) or new generation (avibactam) inhibitors, respectively. Here, access to an azido derivative of the diazabicyclooctane (DBO) scaffold of avibactam for functionalization by the Huisgen–Sharpless cycloaddition reaction is reported. The amoxicillin–DBO combinations were active, indicating that the triazole ring is compatible with drug penetration (minimal inhibitory concentration of 16 μg mL?1 for both species). Mechanistically, β-lactamase inhibition was not sufficient to account for the potentiation of amoxicillin by DBOs. Thus, the latter compounds were investigated as inhibitors of l,d-transpeptidases (Ldts), which are the main peptidoglycan polymerases in mycobacteria. The DBOs acted as slow-binding inhibitors of Ldts by S-carbamoylation indicating that optimization of DBOs for Ldt inhibition is an attractive strategy to obtain drugs selectively active on mycobacteria.

AMINOPIPERIDINE QUINOLINES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY

The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.