79069-15-1Relevant articles and documents
Iterative Synthesis of Stereo- and Sequence-Defined Polymers via Acid-Orthogonal Deprotection Chemistry
He, Wenjing,Li, Maosheng,Tao, Youhua,Wang, Shixue,Wang, Xianhong
supporting information, (2022/01/20)
Absolute control over polymer stereo- and sequence structure is highly challenging in polymer chemistry. Here, an acid-orthogonal deprotection strategy is proposed for the iterative synthesis of a family of unimolecular polymers starting with enantiopure
Synthesis of Enantiomerically Pure 3-Substituted Piperazine-2-acetic Acid Esters as Intermediates for Library Production
Reddy Guduru, Shiva Krishna,Chamakuri, Srinivas,Raji, Idris O.,MacKenzie, Kevin R.,Santini, Conrad,Young, Damian W.
, p. 11777 - 11793 (2018/09/27)
The piperazine heterocycle is broadly exploited in FDA-approved drugs and biologically active compounds, but its chemical diversity is usually limited to ring nitrogen substitutions, leaving the four carbon atoms underutilized. Using an efficient six-step synthesis, chiral amino acids were transformed into 3-substituted piperazine-2-acetic acid esters as diastereomeric mixtures whose cis and trans products (dr 0.56 a? 2.2:1, respectively) could be chromatographically separated. From five amino acids (both antipodes) was obtained a complete matrix of 20 monoprotected chiral 2,3-disubstituted piperazines, each as a single absolute stereoisomer, all but one in multigram quantities. In keeping with our overall purpose of constructing more Csp3-enriched compound libraries for drug discovery, these diverse and versatile piperazines can be functionalized on either nitrogen atom, allowing them to be used as scaffolds for parallel library synthesis and as intermediates for the production of novel piperazine compounds.
LPA5 RECEPTOR AGONIST
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Paragraph 0219; 0220, (2018/07/31)
PROBLEM TO BE SOLVED: To provide a drug containing as an active ingredient a compound having agonist activity for an LPA5 receptor in disease caused by the LPA5 receptor. SOLUTION: A compound represented by general formula (I) in the figure, where all symbols refer to the same as those described in the specification, or a pharmaceutically acceptable salt thereof is useful as a drug component having agonist activity for an LPA5 receptor in prevention and/or treatment of disease caused by the LPA5 receptor, e.g., digestive system disease, immune system disease or cancer. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT