1411975-57-9Relevant academic research and scientific papers
Preparation of N-Substituted N-Arylsulfonylglycines and Their Use in Peptoid Synthesis
Jobin, Steve,Vézina-Dawod, Simon,Herby, Claire,Derson, Antoine,Biron, Eric
, p. 5626 - 5629 (2015)
To increase the chemical diversity accessible with peptoids and peptide-peptoid hybrids, N-alkylated arylsulfonamides were used to prepare side chain protected N-substituted glycines compatible with solid-phase synthesis. The described procedures give acc
N-Substituted arylsulfonamide building blocks as alternative submonomers for peptoid synthesis
Vézina-Dawod, Simon,Derson, Antoine,Biron, Eric
, p. 382 - 385 (2015)
Peptoids (oligo N-substituted glycines) are peptidomimetic oligomers showing attractive structural and pharmacological properties. The efficiency of their synthesis has prompted the use of peptoids in combinatorial libraries. To increase the chemical dive
1,4-DIAZOCANE COMPOUND OR SALT THEREOF
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, (2021/12/03)
A method may produce an isoquinoline-6-sulfonamide derivative useful as a medicinal drug; and an intermediate which is used for the method, and more specifically, a 1,4-diazocane compound of formula (8), wherein R4 is an amino protecting group,
Synthesis of Enantiomerically Pure 5-Substituted Piperazine-2-Acetic Acid Esters as Intermediates for Library Production
Jain, Prashi,Raji, Idris O.,Chamakuri, Srinivas,Mackenzie, Kevin R.,Ebright, Brandon T.,Santini, Conrad,Young, Damian W.
, (2019/05/22)
The piperazine heterocycle is housed within a large number of FDA-approved drugs and biological probe compounds. Structurally, however, these compounds are mostly confined to substitutions on the two ring nitrogen atoms, rationalizing the expansion of piperazine chemical diversity through carbon substitutions. On the basis of the concept of systematic chemical diversity, a divergent six-step synthesis was developed in which chiral amino acids were transformed, with high diastereoselectivity, into either cis or trans 5-substituted piperazine-2-acetic acid esters that could be chromatographically rendered diastereomerically homogeneous. Starting from six commercially available amino acids or their respective amino alcohols (both antipodes), we obtained a complete set of 24 protected chiral 2,5-disubstituted piperazines, as single stereoisomers in multigram quantities. These diverse and versatile piperazines can be functionalized on either nitrogen atom, allowing them to be used as starting materials for parallel library synthesis and as intermediates for the targeted production of more complex C-substituted piperazine compounds.
Synthesis of Enantiomerically Pure 5-Substituted Piperazine-2-Acetic Acid Esters as Intermediates for Library Production
Jain, Prashi,Raji, Idris O.,Chamakuri, Srinivas,MacKenzie, Kevin R.,Ebright, Brandon T.,Santini, Conrad,Young, Damian W.
, p. 6040 - 6064 (2019/05/24)
The piperazine heterocycle is housed within a large number of FDA-approved drugs and biological probe compounds. Structurally, however, these compounds are mostly confined to substitutions on the two ring nitrogen atoms, rationalizing the expansion of piperazine chemical diversity through carbon substitutions. On the basis of the concept of systematic chemical diversity, a divergent six-step synthesis was developed in which chiral amino acids were transformed, with high diastereoselectivity, into either cis or trans 5-substituted piperazine-2-acetic acid esters that could be chromatographically rendered diastereomerically homogeneous. Starting from six commercially available amino acids or their respective amino alcohols (both antipodes), we obtained a complete set of 24 protected chiral 2,5-disubstituted piperazines, as single stereoisomers in multigram quantities. These diverse and versatile piperazines can be functionalized on either nitrogen atom, allowing them to be used as starting materials for parallel library synthesis and as intermediates for the targeted production of more complex C-substituted piperazine compounds.
MANUFACTURING METHOD OF OPTICALLY ACTIVE CARBINOL COMPOUND
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Paragraph 0108; 0114, (2016/11/14)
PROBLEM TO BE SOLVED: To provide a manufacturing method of an optically active carbinol compound having LXRβ activation action and a manufacturing intermediate thereof. SOLUTION: A manufacturing method of an optically active compound represented by the formula (1) comprises manufacturing a 2-(4-(2,5-dimethylpiperazin-1-yl)-3-propylphenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol compound which is an important optically active intermediate. COPYRIGHT: (C)2015,JPOandINPIT
