163877-12-1Relevant articles and documents
Stereoselective process for a CCR3 antagonist
Yue, Tai-Yuen,McLeod, Douglas D.,Albertson, Kevin B.,Beck, Steven R.,Deerberg, Joerg,Fortunak, Joseph M.,Nugent, William A.,Radesca, Lilian A.,Tang, Liya,Xiang, Cathie Dong
, p. 262 - 271 (2012/12/22)
A convergent, multikilogram, stereoselective synthesis of 1 is described. A key fragment, (S)-3-(4-fluorobenzyl)piperidine (2) was synthesized from valerolactam in three steps using our recently discovered Ir-BDPP-catalyzed asymmetric hydrogenation. Anoth
Asymmetric synthesis of a new helix-forming β-amino acid: trans-4-aminopiperidine-3-carboxylic acid
Schinnerl, Marina,Murray, Justin K.,Langenhan, Joseph M.,Gellman, Samuel H.
, p. 721 - 726 (2007/10/03)
We report a synthesis of a protected derivative of trans-4aminopiperidine-3-carboxylic acid (APiC). The route provides either enantiomer. All intermediates are purified by crystallization, and large-scale preparation is therefore possible. An analogous ro
Stereoselective reduction of enantiopure β-enamino esters by hydride: A convenient synthesis of both enantiopure β-amino esters
Cimarelli, Cristina,Palmieri, Gianni
, p. 5557 - 5563 (2007/10/03)
The reduction of enantiopure β-enamino esters 1 with sodium triacetoxyborohydride in acetic acid is described. This occurs with good diastereo- and enantioselectivity to yield β-amino esters 2 and 3 (after hydrogenolysis of the N-chiral group). A model is