144261-18-7Relevant academic research and scientific papers
4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors
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, (2008/06/13)
This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.
Enzymatic resolution of benzothiazepine for the preparation of squalene synthetase inhibitors
Yang, Xiaojing,Buzon, Leanne,Hamanaka, Ernie,Liu, Kevin K.-C.
, p. 4447 - 4450 (2007/10/03)
A key intermediate with a 4,1-benzothiazepine skeleton, useful for the synthesis of potent squalene synthetase inhibitors, has been prepared via enzymatic resolution providing excellent yield and enantiomeric purity.
Naphthyl-benzoxazepines or -benzothiazepines as squalene synthetase inhibitors
-
, (2008/06/13)
This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents and antiatheroscierosis agents.
Bimolecular Nucleophilic Substitution (SN2) Reactions of Neopentyl Arenesulfonates with Anilines and Benzylamines in Methanol
Koh, Han Joong,Lee, Hai Whang,Lee, Ikchoon
, p. 253 - 258 (2007/10/02)
Bimolecular nucleophilic substitution (SN2) reactions of neopentyl arenesulfonates with anilines and benzylamines in methanol at 55.0 deg C are reported.The tightness of the transition state (TS) is similar to that for other typical SN2 processes at a primary alkyl carbon centre based on the magnitude of the cross-interaction constant ρxz (0.30) between the substituents in the nucleophile (X) and leaving group (Z).The TS variation is in accord with that predicted by the potential energy surface diagram, which in turn is consistent with the positive sign of ρxz; a later TS is obtained with a weaker nucleophile and nucleofuge.Taft's polar substituent constant, ?*, for the trimethylsilyl group is estimated to be -0.48 by using a factor of 1.875 for the fall-off of ?* from the tert-butyl to the neopentyl group and extrapolating from the experimental Taft plot.
