- Combined Photoredox/Enzymatic C?H Benzylic Hydroxylations
-
Chemical transformations that install heteroatoms into C?H bonds are of significant interest because they streamline the construction of value-added small molecules. Direct C?H oxyfunctionalization, or the one step conversion of a C?H bond to a C?O bond, could be a highly enabling transformation due to the prevalence of the resulting enantioenriched alcohols in pharmaceuticals and natural products,. Here we report a single-flask photoredox/enzymatic process for direct C?H hydroxylation that proceeds with broad reactivity, chemoselectivity and enantioselectivity. This unified strategy advances general photoredox and enzymatic catalysis synergy and enables chemoenzymatic processes for powerful and selective oxidative transformations.
- Betori, Rick C.,May, Catherine M.,Scheidt, Karl A.
-
supporting information
p. 16490 - 16494
(2019/11/03)
-
- Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: A case of clofilium analogues
-
Cardiotoxicity is a side effect that plagues modern drug design and is very often due to the off-target blockade of the human ether-à-go-go related gene (hERG) potassium channel. To better understand the structural determinants of this blockade, we design
- Louvel, Julien,Carvalho, Jo?o F.S.,Yu, Zhiyi,Soethoudt, Marjolein,Lenselink, Eelke B.,Klaasse, Elisabeth,Brussee, Johannes,Ijzerman, Adriaan P.
-
supporting information
p. 9427 - 9440
(2014/01/06)
-
- Diaryl piperidines as CB1 receptor antagonists
-
The syntheses and SAR investigations of novel CB1 receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO m
- Scott, Jack D.,Li, Sarah W.,Wang, Hongwu,Xia, Yan,Jayne, Charles L.,Miller, Michael W.,Duffy, Ruth A.,Boykow, George C.,Kowalski, Timothy J.,Spar, Brian D.,Stamford, Andrew W.,Chackalamannil, Samuel,Lachowicz, Jean E.,Greenlee, William J.
-
scheme or table
p. 1278 - 1283
(2010/06/15)
-
- Diaryl piperidines as CB1 modulators
-
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
- -
-
Page/Page column 75-76
(2010/11/28)
-
- Synthesis and biological activity of novel 5-(omega-aryloxyalkyl)oxazole derivatives as brain-derived neurotrophic factor inducers.
-
A novel series of 5-(omega-aryloxyalkyl)oxazole derivatives was prepared and their effects on brain-derived neurotrophic factor (BDNF) production were evaluated in human neuroblastoma (SK-N-SH) cells. Syntheses were performed by construction of an oxazole
- Maekawa, Tsuyoshi,Sakai, Nozomu,Tawada, Hiroyuki,Murase, Katsuhito,Hazama, Masatoshi,Sugiyama, Yasuo,Momose
-
p. 565 - 573
(2007/10/03)
-
- Tetracyclic compound
-
This invention relates to a novel tetracyclic compound represented by formula (I): STR1 or its pharmacologically-acceptable salt. The compound of this invention has strong immunosuppressive activity, and is useful as an immunosuppressive agent and as an a
- -
-
-
- Preparation and Reactivities of (η3-1- and 2-Trimethylsiloxyallyl)Fe(CO2)NO Complexes. Intermediates Functioning as Equivalents of β- and α-Acyl Carbocations and Acyl Carbanions
-
(η3-1- and 2-Trimethylsiloxyallyl)Fe(CO)2NO complexes were prepared by the reaction of the corresponding siloxyallylic halides with Bu4N.These complexes reacted with both of carbon nucleophiles and carbon electrophiles preferentially at the less hindered sites of the allylic ligands.In these reactions, (η3-1-trimethylsiloxyallyl)Fe(CO)2NO complexes served as synthetically equivalent synthons for both of β-acyl carbocations and β-acyl carbanions and (η3-2-trimethylsiloxyallyl)Fe(CO)2NO complexes as both of α-acyl carbocations and α-acyl carbanions.The stereochemical courses of the reactions are described.
- Itoh, Keiji,Nakanishi, Saburo,Otsuji, Yoshio
-
p. 2965 - 2977
(2007/10/02)
-