905306-11-8

Usage

Uses

Used in Pharmaceutical Research:
2-Oxa-5-azabicyclo[2.2.1]heptane-5-carboxylic acid, 1,1-diMethylethyl ester, (1S,4S)is used as a building block in pharmaceutical research for the preparation of various pharmaceutical compounds and potential drug candidates. Its unique bicyclic structure and ester functionality make it a valuable component in the development of new therapeutic agents.
Used in Organic Synthesis:
In the field of organic synthesis, 2-Oxa-5-azabicyclo[2.2.1]heptane-5-carboxylic acid, 1,1-diMethylethyl ester, (1S,4S)serves as a versatile intermediate for the synthesis of complex organic molecules. Its reactivity and stereochemistry can be exploited to construct a wide range of target compounds, making it a valuable tool for chemists in various applications.

Upstream product

• 2584-71-6 cis-hydroxy-D-proline 
• 387362-68-7 tert-butyl 4-hydroxy-2-(hydroxymethyl)pyrrolidine-1-formate 
• 114760-51-9 (2R,4R)-1-(tert-butixycarbonyl)-4-<(tert-butyldimethylsilyl)oxy>-2-carbomethoxypyrrolidine 
• 114676-58-3 (2R,4R)-tert-butyl 4-((tert-butyldimethylsilyl)oxy)-2-(hydroxymethyl)pyrrolidine-1-carboxylate 
• 114676-69-6 (2R,4R)-1-tert-butyl 2-methyl 4-hydroxypyrrolidine-1,2-dicarboxylate 
• 114676-60-7 (2R,4R)-4-(tert-Butyl-dimethyl-silanyloxy)-2-methanesulfonyloxymethyl-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 393810-24-7 (3R,5S)-3-fluoro-5-hydroxymethyl-2-pyrrolidinone 
• 24424-99-5 di-tert-butyl dicarbonate 
• 791602-93-2 (2S,4S)-4-[[(1,1-dimethylethyl)dimethylsilyl]oxy]-2-(hydroxymethyl)-1-pyrrolidinecarboxylic acid 1,1-dimethylethyl ester 
• 367966-45-8 (2S,4S)-4-[[(1,1-dimethylethyl)dimethylsilyl]oxy]-1,2-pyrrolidinedicarboxylic acid 1-(1,1-dimethylethyl) 2-methyl ester 
• 74844-91-0 (2S,4S)-N-tert-butoxycarbonyl-4-hydroxyproline methyl ester 
• 114676-59-4 (2R,4R)-4-hydroxy-2-methoxycarbonylpyrrolidine hydrochloride 

Relevant academic research and scientific papers

Synthesis of Chiral Azabicycles from Pyroglutaminols

The stereocontrolled synthesis of a range of substituted bicyclic morpholine and piperazine derivatives is reported from substituted pyroglutaminols via an intramolecular SN2 cyclization as the key step. This enantiospecific approach toward chiral bicyclic morpholines and piperazines offers new opportunities to access these challenging ring systems, which are becoming increasingly common motifs in drug discovery.

As Aurora kinase inhibitor derivatives

The present invention relates to a substituted pyrazole derivative used for inhibiting Aurora kinase and represented by formula (I) or formula (Ia), or stereo isomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, esters, pharmaceutically acceptable salts or prodrugs thereof, a medicinal composition containing the above compounds as active ingredients, and a use of the compounds and the medicinal composition in preparation of medicines for protecting, processing, treating or mitigating proliferative diseases of patients.

PI3K kinase inhibitor, to pharmaceutical compositions comprising the same and application thereof

The invention discloses a phosphoinositide 3-kinase (P13K) inhibitor, a pharmaceutical composition containing the P13K inhibitor, and application of the P13K inhibitor and the pharmaceutical composition. The P13K inhibitor comprises a pyrimidine compound and a stereoisomer/hydrate/pharmaceutically-acceptable salt thereof. The pyrimidine compound has a general formula I of which the structure is shown in the specification. The P13K inhibitor and the pharmaceutical composition containing the same can be used for inhibiting PI3 Ks and treating proliferative diseases on which the PI3 Ks act. According to the invention, high-effectiveness and high-selectivity inhibitors for treating proliferative diseases on which PI3Ks act can be provided.

AMINO-TETRAZOLES ANALOGUES AND METHODS OF USE

A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R 5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.

Design, Synthesis, and Properties of (4S)-7-(4-Amino-2-substituted-pyrrolidin-1-yl)quinolone-3-carboxylic Acids

The quinolinecarboxylic acids constitute a class of extremely potent and orally active broad-spectrum antibacterial agents.These compounds have been shown to inhibit DNA gyrase, a key enzyme in bacterial DNA replication.The 7-(3-aminopyrrolidinyl)quinolone A-60969 (1) is a particularly potent member of this class and is currently undergoing clinical evaluation.We have studied a series of enantiomerically homogeneous (4S)-7-(4-amino-2-substituted-pyrrolidinyl)quinolones in an effort to utilize the 2-position of the pyrrolidine moiety to improve upon the solubility and pharmacokinetic properties of this class of compounds while still maintaining potent antibacterial activity.We have found that the absolute stereochemistry at the 2-position of the pyrrolydine ring is critical to the maintenance of such activity.In this paper, we report the full details of the asymmetric synthesis and the in vitro and in vivo structure-activity relationships of this series of compounds as well as the physiochemical properties, such as water solubility and log P, associated with the structural modifications.We also discuss the pharmacokinetic properties of several of these compounds in mice and the pharmacokinetics of 59, which has the best overall properties of agents in this study, in dog.