873693-47-1Relevant articles and documents
Application of [BoPhoz Rh] catalysts in the asymmetric hydrogenation of a pyridyl benzothiophene alkene
Gross, Timothy,Chou, Shine,Dyke, Alan,Dominguez, Beatriz,Groarke, Michelle,Medlock, Jonathan,Ouellette, Michael,Reddy, Jayachandra P.,Seger, Andreas,Zook, Scott,Zanotti-Gerosa, Antonio
experimental part, p. 1025 - 1028 (2012/03/27)
The asymmetric hydrogenation of a pyridyl benzothiophene alkene has been successfully accomplished using [BoPhoz Rh] catalysts. By tailoring the steric properties of the BoPhoz ligand, the ee of the product could be increased from just 12% to 90%. This research further expands the substrate scope of the conventional class of functionalized alkenes amenable to catalytic asymmetric hydrogenation.
Novel benzothiophene H1-antihistamines for the treatment of insomnia
Moree, Wilna J.,Jovic, Florence,Coon, Timothy,Yu, Jinghua,Li, Bin-Feng,Tucci, Fabio C.,Marinkovic, Dragan,Gross, Raymond S.,Malany, Siobhan,Bradbury, Margaret J.,Hernandez, Lisa M.,O'Brien, Zhihong,Wen, Jianyun,Wang, Hua,Hoare, Samuel R.J.,Petroski, Robert E.,Sacaan, Aida,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
scheme or table, p. 2316 - 2320 (2010/09/05)
SAR of lead benzothiophene H1-antihistamine 2 was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-li
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia
Moree, Wilna J.,Li, Bin-Feng,Jovic, Florence,Coon, Timothy,Yu, Jinghua,Gross, Raymond S.,Tucci, Fabio,Marinkovic, Dragan,Zamani-Kord, Said,Malany, Siobhan,Bradbury, Margaret J.,Hernandez, Lisa M.,O'Brien, Zhihong,Wen, Jianyun,Wang, Hua,Hoare, Samuel R. J.,Petroski, Robert E.,Sacaan, Aida,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
supporting information; experimental part, p. 5307 - 5310 (2010/06/13)
Analogues of the known H1-antihistamine R-dimethindene were profiled as potential agents for the treatment of insomnia. Several highly selective compounds were efficacious in rodent sleep models. On the basis of overall profile, indene 1d and benzothiophene 2a had pharmacokinetic properties suitable for evaluation in night time dosing. Compound 2a did not show an in vivo cardiovascular effect from weak hERG channel inhibition.
Chemical development of NBI-75043. Use of a flow reactor to circumvent a batch-limited metal#halogen exchange reaction
Gross, Timothy D.,Chou, Shine,Bonneville, Daniel,Gross, Raymond S.,Wang, Peng,Campopiano, Onorato,Ouellette, Michael A.,Zook, Scott E.,Reddy, Jayachandra P.,Moree, Wilna J.,Jovic, Florence,Chopade, Shubham
, p. 929 - 939 (2013/01/03)
The discovery route and subsequent scale-up routes for NBI-75043 are presented. When traditional batch chemistry was found to limit the scale of a key reaction, a flow reactor was designed and optimized to provide an alternate method of production.
Sleep inducing compounds and methods relating thereto
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Page/Page column 24-25, (2010/02/15)
Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.