1403898-70-3

Usage

Uses

Used in Medicinal Chemistry:
(2R,5R)-2-hydroxymethyl-5-methylpiperazine-1,4-dicarboxylic acid 1-benzyl ester 4-tert-butyl ester is utilized as a key intermediate in the synthesis of various pharmaceutical compounds. Its unique structure and functional groups make it a valuable building block for the development of new drugs with specific therapeutic targets.
Used in Organic Synthesis:
In the field of organic synthesis, (2R,5R)-2-hydroxymethyl-5-methylpiperazine-1,4-dicarboxylic acid 1-benzyl ester 4-tert-butyl ester serves as a versatile reactant for the creation of a wide range of organic molecules. Its ester and carboxylic acid groups can participate in numerous chemical reactions, facilitating the synthesis of complex organic compounds.
Used in Pharmaceutical Formulations:
(2R,5R)-2-hydroxymethyl-5-methylpiperazine-1,4-dicarboxylic acid 1-benzyl ester 4-tert-butyl ester is employed as a component in pharmaceutical formulations to enhance the solubility, stability, and bioavailability of active pharmaceutical ingredients. Its ability to modify reactivity and solubility makes it a useful excipient in the development of effective drug delivery systems.
Further research and analysis are necessary to fully understand the capabilities and effects of (2R,5R)-2-hydroxymethyl-5-methylpiperazine-1,4-dicarboxylic acid 1-benzyl ester 4-tert-butyl ester in these applications and to discover additional uses across various industries.

Upstream product

• 1403898-64-5 (2R,5R)-5-(hydroxymethyl)-2-methylpiperazine-1-carboxylic acid tert-butyl ester 
• 501-53-1 benzyl chloroformate 
• 1403898-62-3 (3S,6R)-3-(hydroxymethyl)-6-methylpiperazine-2,5-dione 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 1403900-65-1 (2R,5R)-4-[2-(6-benzyl-3,3-dimethyl-2,3-dihydro-pyrrolo-[3,2-c]pyridin-1-yl)-2-oxo-ethyl]-5-methoxymethyl-2-methyl-piperazine-1-carboxylic acid tert-butyl ester 
• 1403896-55-8 1-(6-benzyl-3,3-dimethyl-2,3-dihydro-pyrrolo[3,2-c]-pyridin-1-yl)-2-((2R,5R)-2-methoxymethyl-5-methyl-piperazin-1-yl)-ethanone hydrochloride 
• 1403898-73-6 (2R,5R)-4-benzyloxycarbonylmethyl-5-methoxymethyl-2-methyl-piperazine-1-carboxylicacid tert-butyl ester 
• 1403898-71-4 (2R,5R)-2-methoxymethyl-5-methyl-piperazine-1,4-dicarboxylic acid 1-benzyl ester 4-tertbutylester 
• 2349395-78-2 1-tert-butyl 3-methyl (3R,6R)-6-methylpiperazine-1,3-dicarboxylate 

Relevant academic research and scientific papers

Structure-based design and pharmacokinetic optimization of covalent allosteric inhibitors of the mutant gtpase krasg12c

Attempts to directly drug the important oncogene KRAS have met with limited success despite numerous efforts across industry and academia. The KRASG12C mutant represents an "Achilles heel" and has recently yielded to covalent targeting with small molecules that bind the mutant cysteine and create an allosteric pocket on GDP-bound RAS, locking it in an inactive state. A weak inhibitor at this site was optimized through conformational locking of a piperazine-quinazoline motif and linker modification. Subsequent introduction of a key methyl group to the piperazine resulted in enhancements in potency, permeability, clearance, and reactivity, leading to identification of a potent KRASG12C inhibitor with high selectivity and excellent cross-species pharmacokinetic parameters and in vivo efficacy.

CHEMICAL COMPOUNDS

The specification relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.

Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP

(Figure Presented) Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with tumor genesis and tumor growth. IAPs have been proposed as targets for anticanc

BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY

The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.