184844-98-2

Usage

Uses

Used in Pharmaceutical Research:
((3R,4R)-1-benzyl-4-(trifluoromethyl)pyrrolidin-3-yl)methanol is utilized as a building block in pharmaceutical research for its potential to contribute to the creation of diverse drug-like compounds. Its unique structure and functional groups allow for the development of new therapeutic agents that can be tailored to target specific biological pathways or diseases.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, ((3R,4R)-1-benzyl-4-(trifluoromethyl)pyrrolidin-3-yl)methanol serves as a key component in the design and synthesis of novel compounds with potential medicinal properties. Its stereochemistry and functional groups are instrumental in studying how these compounds interact with biological targets, thereby aiding in the optimization of drug candidates.
Used in Biological Imaging:
((3R,4R)-1-benzyl-4-(trifluoromethyl)pyrrolidin-3-yl)methanol is also used in biological imaging as a tool to study the distribution, metabolism, and activity of drug-like compounds within biological systems. Its unique properties can help visualize and understand the behavior of these compounds, providing insights into their potential therapeutic applications.
Used in Organic Synthesis:
As a building block in organic synthesis, ((3R,4R)-1-benzyl-4-(trifluoromethyl)pyrrolidin-3-yl)methanol is employed for the synthesis of complex organic molecules. Its versatility and the presence of distinct functional groups make it suitable for a wide range of synthetic applications, contributing to the development of new chemical entities with various applications.

Upstream product

• 217096-03-2 trans-1-benzyl-4-trifluoromethylpyrrolidine-3-carboxylic acid ethyl ester 

Downstream Products

• 1817633-15-0 tert-butyl (3R,4R)-3-(hydroxymethyl)-4-(trifluoromethyl)pyrrolidine-1-carboxylate 

Relevant academic research and scientific papers

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately, these patients' disease progresses, often driven by a second-site mutation in the EGFR kinase domain (T790M). Another liability of the first generation drugs is severe adverse events driven by inhibition of WT EGFR. As such, our goal was to develop a highly potent irreversible inhibitor with the largest selectivity ratio between the drug-resistant double mutants (L858R/T790M, Del/T790M) and WT EGFR. A unique approach to develop covalent inhibitors, optimization of reversible binding affinity, served as a cornerstone of this effort. PF-06459988 was discovered as a novel, third generation irreversible inhibitor, which demonstrates (i) high potency and specificity to the T790M-containing double mutant EGFRs, (ii) minimal intrinsic chemical reactivity of the electrophilic warhead, (iii) greatly reduced proteome reactivity relative to earlier irreversible EGFR inhibitors, and (iv) minimal activity against WT EGFR.

Quinolinecarboxylic acid derivatives and salts thereof

Quinolinecarboxylic acid derivatives which are represented by the general formula (I) STR1 wherein R1 is a C1 to C6 alkyl group which may be substituted, a C2 to C6 alkenyl group which may be substituted, a C3 to C7 cycloalkyl group which my be substituted or an aryl group which may be substituted, R2 is hydrogen atom; a halogen atom; hydroxyl group which may be protected, amino group or a C1 to C6 alkylamino group each of which may be protected; a C1 to C6 dialkylamino group or a C1 to C6 alkyl group, R3 is hydrogen atom or a C1 to C6 alkyl group, A is nitrogen atom or STR2 wherein A' is hydrogen atom. a halogen atom, a C1 to C6 alkyl group, a C1 to C6 alkoxyl group which may be substituted, cyano group, or nitro group, and A' may form a ring with R1 ; the ring may include oxygen atom, nitrogen atom, or sulfur atom as a constituent atom; the ring may be substituted with a C1 to C6 alkyl group, X is hydroxymethyl group; aminomethyl group or amino group each of which may be protected, and salts thereof, and antibacterial agents which comprise the quinolinecarboxylic acid derivatives and salts thereof as active ingredients, and therapeutical methods thereby.