200184-53-8Relevant articles and documents
Asymmetric lithiation trapping of N -boc heterocycles at temperatures above -78°C
Gelardi, Giacomo,Barker, Graeme,O'Brien, Peter,Blakemore, David C.
supporting information, p. 5424 - 5427 (2013/11/19)
The asymmetric lithiation trapping of N-Boc heterocycles using s-BuLi/chiral diamines at temperatures up to -20°C is reported. Depending on the N-Boc heterocycle, lithiation is accomplished using s-BuLi and (-)-sparteine or the (+)-sparteine surrogate in the temperature range -50 to -20°C for short reaction times (2-20 min). Subsequent electrophilic trapping or transmetalation-Negishi coupling delivered functionalized N-Boc heterocycles in 47-95% yield and 77:23-93:7 er. With N-Boc pyrrolidine, trapped products can be generated in ~90:10 er even at -20°C.
Aromatic amidine derivatives useful as selective thrombin inhibitors
-
, (2008/06/13)
The present invention relates to a novel thrombin inhibitor which is effective even when orally administered. More specifically, the present invention relates to an aromatic amidine derivative represented by formula (I) and the salts thereof, which show potent selective inhibitory activity for thrombin in which (a), R, R1, R2, R3, A, W, Y and n are defined as described in the specification.
Catalytic asymmetric hydrogenation of 1-aza-2-cycloalkene-2-carboxylates catalyzed by a trans-chelating chiral diphosphine PhTRAP-rhodium complex
Kuwano, Ryoichi,Karube, Daisuke,Ito, Yoshihiko
, p. 9045 - 9049 (2007/10/03)
A rhodium complex coordinated with a trans-chelating chiral diphosphine (S,S)-(R,R)-PhTRAP was an effective catalyst for asymmetric hydrogenation of N-acyl-1-aza-2-cycloalkene-2-carboxylates, which gave the corresponding protected cyclic α-amino acids wit