790223-47-1Relevant academic research and scientific papers
CARBAMOYL PHENYLALANINOL ANALOGS AND USES THEREOF
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Paragraph 0090, (2019/02/15)
The present invention relates to carbamoyl phenylalaninol analogs and methods of using the same to treat disorders.
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.
Efficient synthesis of functionalized olefins by Wittig reaction using Amberlite resin as a mild base
Valkute, Tushar R.,Aratikatla, Eswar K.,Bhattacharya, Asish K.
, p. 581 - 589 (2017/03/15)
A convenient procedure for the synthesis of olefins by the reaction of stabilized, semistabilized, and nonstabilized phosphorous ylides with various aldehydes or ketone using Amberlite resin as a mild base is described. Our developed method offers facile and racemization-free synthesis of α,β-unsaturated amino esters and chiral allylic amine. The developed methodology offers mild reaction conditions, high efficiency, and facile isolation of the final products, a practical alternative to known procedures.
Practical approach for asymmetric hydroxyamination of aldehydes with in situ generated nitrosocarbonyl compounds: Application to one-pot synthesis of chiral allylamines
Kano, Taichi,Shirozu, Fumitaka,Maruoka, Keiji
, p. 1530 - 1532 (2014/04/03)
The highly regio- and enantioselective hydroxyamination of aldehydes with in situ generated nitrosocarbonyl compounds from a hydroxamic acid derivative was realized by simple and readily available chiral amine catalysts. The resulting hydroxyamination products were readily converted to the corresponding chiral 1,2-aminoalcohol or allylamine derivatives in one pot.
Highly selective synthesis of enantiopure (S,E)-α,β-unsaturated γ-amino esters through a sequential reaction of ethyl dibromoacetate with α-amino aldehydes promoted by chromium dichloride
Concellon, Jose M.,Mejica, Carmen
, p. 5250 - 5255 (2008/03/30)
A sequential reaction of ethyl dibromoacetate with various enantiopure N,N-dibenzyl- or N-Boc-α-amino aldehydes (derived from natural α-amino acids), promoted by chromium dichloride, afforded optically active (S,E)-α,β-unsaturated γ-amino esters. The C=C
NK-2 ANTAGONIST BASIC LINEAR COMPOUNDS AND FORMULATIONS CONTAINING THEM
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Page 10-11, (2010/02/09)
The present invention describes compounds with formula (I) having linear structure basic properties useful as NK-2 antagonists; pharmaceutical compositions containing said compounds are also described and processes for their preparation.
