514843-72-2Relevant academic research and scientific papers
Selective Hydrogen Atom Abstraction through Induced Bond Polarization: Direct α-Arylation of Alcohols through Photoredox, HAT, and Nickel Catalysis
Twilton, Jack,Christensen, Melodie,DiRocco, Daniel A.,Ruck, Rebecca T.,Davies, Ian W.,MacMillan, David W. C.
supporting information, p. 5369 - 5373 (2018/04/09)
The combination of nickel metallaphotoredox catalysis, hydrogen atom transfer catalysis, and a Lewis acid activation mode, has led to the development of an arylation method for the selective functionalization of alcohol α-hydroxy C?H bonds. This approach employs zinc-mediated alcohol deprotonation to activate α-hydroxy C?H bonds while simultaneously suppressing C?O bond formation by inhibiting the formation of nickel alkoxide species. The use of Zn-based Lewis acids also deactivates other hydridic bonds such as α-amino and α-oxy C?H bonds. This approach facilitates rapid access to benzylic alcohols, an important motif in drug discovery. A 3-step synthesis of the drug Prozac exemplifies the utility of this new method.
Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl) carbonyl]-4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)-phenyl}ethyl-3(S) -methyl-1-piperazinyl]-4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Sel
Tagat, Jayaram R.,McCombie, Stuart W.,Nazareno, Dennis,Labroli, Marc A.,Xiao, Yushi,Steensma, Ruo W.,Strizki, Julie M.,Baroudy, Bahige M.,Cox, Kathleen,Lachowicz, Jean,Varty, Geoffrey,Watkins, Robert
, p. 2405 - 2408 (2007/10/03)
The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs M1, M2) and potency in the title compounds. Optimization of the lead benzylic methyl compound 3 led to the methoxymethyl analogue 30,
17-Beta hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
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Page 19, (2010/02/05)
There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17β-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.
