41807-59-4Relevant articles and documents
Utilization of a Trimethylsilyl Group as a Synthetic Equivalent of a Hydroxyl Group via Chemoselective C(sp3)-H Borylation at the Methyl Group on Silicon
Torigoe, Takeru,Ohmura, Toshimichi,Suginome, Michinori
, p. 2943 - 2956 (2017/03/23)
A conversion of trimethylsilylalkanes into the corresponding alcohols is established based on an iridium-catalyzed, chemoselective C(sp3)-H borylation of the methyl group on silicon. The (borylmethyl)silyl group formed by C(sp3)-H borylation is treated with H2O2/NaOH, and the resulting (hydroxymethyl)silyl group is converted into a hydroxyl group by Brook rearrangement, followed by oxidation of the resulting methoxysilyl group under Tamao conditions. An alternative route proceeding through the formylsilyl group formed from a (hydroxymethyl)silyl group by Swern oxidation is also established. The method is applicable to substituted trimethylsilylcycloalkanes and 1,1-dimethyl-1-silacyclopentane for conversion into the corresponding stereodefined cycloalkyl alcohols and 1,4-butanediol.
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists
He, Shuwen,Dobbelaar, Peter H.,Liu, Jian,Jian, Tianying,Sebhat, Iyassu K.,Lin, Linus S.,Goodman, Allan,Guo, Cheng,Guzzo, Peter R.,Hadden, Mark,Henderson, Alan J.,Ruenz, Megan,Sargent, Bruce J.,Yet, Larry,Kelly, Theresa M.,Palyha, Oksana,Kan, Yanqing,Pan, Jie,Chen, Howard,Marsh, Donald J.,Shearman, Lauren P.,Strack, Alison M.,Metzger, Joseph M.,Feighner, Scott D.,Tan, Carina,Howard, Andrew D.,Tamvakopoulos, Constantin,Peng, Qianping,Guan, Xiao-Ming,Reitman, Marc L.,Patchett, Arthur A.,Wyvratt Jr., Matthew J.,Nargund, Ravi P.
scheme or table, p. 1913 - 1917 (2010/07/02)
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.
