111604-99-0Relevant articles and documents
Fluoride-catalyzed Michael addition of nitrotoluenes to activated α, β-unsaturated esters
Li, Wen-Sen,Thottathil, John,Murphy, Michael
, p. 6591 - 6594 (2007/10/02)
We have found that in the presence of fluoride ion, nitrotoluenes of type 1 undergo Michael addition to activated α, β-unsaturated esters of type 2 in good to excellent yield (Scheme 1). The generality and limitation of this reaction and its application t
Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones
Floyd,Kimball,Krapcho,Das,Turk,Moquin,Lago,Duff,Lee,White,Ridgewell,Moreland,Brittain,Normandin,Hedberg,Cucinotta
, p. 756 - 772 (2007/10/02)
As part of a program to discover potent antihypertensive analogues of diltiazem (3a), we prepared 1-benzazepin-2-ones (4). Benzazepinones competitively displace radiolabeled diltiazem, and show the same absolute stereochemical preferences at the calcium channel receptor protein. Derivatives of 4 containing a trifluoromethyl substituent in the fused aromatic ring show potent and long-acting antihypertensive activity. Studies of the metabolism of 4 lead to the metabolically stable antihypertensive calcium channel blockers 5a and 5c. Benzazepinone 5a is a longer acting and more potent antihypertensive agent than the second generation diltiazem analogue TA-3090 (3e).
Process for benzazepine intermediates
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, (2008/06/13)
A process is disclosed for providing benzazepine intermediates of the formulae STR1 wherein R3, R4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine de