Search Results - "Dixon, Darryl D"
-
1
A New Reagent for Direct Difluoromethylation
Published in Journal of the American Chemical Society (25-01-2012)“…Molecular scaffolds containing alkylfluorine substituents are desired in many areas of chemical research from materials to pharmaceuticals. Herein, we report…”
Get full text
Journal Article -
2
Practical and innate carbon–hydrogen functionalization of heterocycles
Published in Nature (London) (06-12-2012)“…It is shown that zinc sulphinate salts can be used to transfer alkyl radicals to heterocycles, allowing for the mild, direct and operationally simple formation…”
Get full text
Journal Article -
3
CH Functionalization Logic Enables Synthesis of (+)-Hongoquercin A and Related Compounds
Published in Angewandte Chemie International Edition (08-07-2013)“…The specifics: A synthesis of the sesquiterpenoid antibiotic (+)‐hongoquercin A using sequential site‐specific CH methylation and oxidation reactions is…”
Get full text
Journal Article -
4
The Evolution of the Total Synthesis of Rocaglamide
Published in Chemistry : a European journal (24-10-2016)“…The complex flavagline, (−)‐rocaglamide, possesses a synthetically intriguing tricyclic scaffold with five contiguous stereocenters and also exhibits potent…”
Get full text
Journal Article -
5
Redox-Active Esters in Fe-Catalyzed C–C Coupling
Published in Journal of the American Chemical Society (07-09-2016)“…Cross-couplings of alkyl halides and organometallic species based on single electron transfer using Ni and Fe catalyst systems have been studied extensively,…”
Get full text
Journal Article -
6
C3-Heteroaroyl cannabinoids as photolabeling ligands for the CB2 cannabinoid receptor
Published in Bioorganic & medicinal chemistry letters (15-08-2012)“…A series of tricyclic cannabinoids incorporating a heteroaroyl group at C3 were prepared as probes to explore the binding site(s) of the CB1 and CB2 receptors…”
Get full text
Journal Article -
7
Practical Radical Cyclizations with Arylboronic Acids and Trifluoroborates
Published in Organic letters (21-10-2011)“…Practical radical cyclizations using organoboronic acids and trifluoroborates take place in water, open to air, and in a scalable fashion employing catalytic…”
Get full text
Journal Article -
8
3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma
Published in Journal of medicinal chemistry (08-08-2019)“…The hypoxia-inducible factor 2α (HIF-2α) is a key oncogenic driver in clear cell renal cell carcinoma (ccRCC). Our first HIF-2α inhibitor PT2385 demonstrated…”
Get full text
Journal Article -
9
A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma
Published in Cancer research (Chicago, Ill.) (15-09-2016)“…More than 90% of clear cell renal cell carcinomas (ccRCC) exhibit inactivation of the von Hippel-Lindau (pVHL) tumor suppressor, establishing it as the major…”
Get full text
Journal Article -
10
Scalable, Divergent Synthesis of Meroterpenoids via “Borono-sclareolide”
Published in Journal of the American Chemical Society (23-05-2012)“…A scalable, divergent synthesis of bioactive meroterpenoids has been developed. A key component of this work is the invention of “borono-sclareolide”, a…”
Get full text
Journal Article -
11
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Published in Journal of medicinal chemistry (08-11-2018)“…HIF-2α, a member of the HIF family of transcription factors, is a key oncogenic driver in cancers such as clear cell renal cell carcinoma (ccRCC). A signature…”
Get full text
Journal Article -
12
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)‑3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro‑1H‑inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Published in Journal of medicinal chemistry (08-11-2018)“…HIF-2α, a member of the HIF family of transcription factors, is a key oncogenic driver in cancers such as clear cell renal cell carcinoma (ccRCC). A signature…”
Get full text
Journal Article -
13
Direct Lewis Acid Catalyzed Conversion of Enantioenriched N‑Acyloxazolidinones to Chiral Esters, Amides, and Acids
Published in Journal of organic chemistry (07-12-2018)“…The identification of Yb(OTf)3 through a multivariable high-throughput experimentation strategy has enabled a unified protocol for the direct conversion of…”
Get full text
Journal Article -
14
Revisiting the Cleavage of Evans Oxazolidinones with LiOH/H2O2
Published in Organic process research & development (19-07-2019)“…The use of LiOH/H2O2 for cleavage of Evans oxazolidinones is an essential but often overlooked part of using these ubiquitous chiral auxiliaries in synthetic…”
Get full text
Journal Article -
15
Rapid Development of a Commercial Process for Linrodostat, an Indoleamine 2,3-Dioxygenase (IDO) Inhibitor
Published in Organic process research & development (15-11-2019)“…The process development and the kilogram-scale synthesis of linrodostat (BMS-986205, 1) are described. The synthesis features several highly efficient…”
Get full text
Journal Article -
16
Safe Scale-up of an Oxygen-Releasing Cleavage of Evans Oxazolidinone with Hydrogen Peroxide
Published in Organic process research & development (21-02-2020)“…In the pharmaceutical industry, H2O2-mediated oxidation reactions are commonly used in chemical syntheses but they can also introduce unexpected safety…”
Get full text
Journal Article -
17
A Mild, Functional Group Tolerant Addition of Organozinc Nucleophiles to N‑Activated Quinolines and Isoquinolines
Published in Journal of organic chemistry (06-10-2017)“…An addition of organozinc nucleophiles to N-acyl activated quinolines and isoquinolines is described. Simple transmetalation with the corresponding Grignard…”
Get full text
Journal Article -
18
A simple procedure for C–C bond cleavage of aromatic and aliphatic epoxides with aqueous sodium periodate under ambient conditions
Published in Tetrahedron letters (21-04-2008)“…The sodium periodate mediated oxidative cleavage of the C–C bond of 12 epoxides is reported with yields of the corresponding carbonyl compounds in up to 91%…”
Get full text
Journal Article -
19
Heteroadamantyl Cannabinoids
Published in Journal of medicinal chemistry (12-08-2010)“…The aliphatic side chain plays a pivotal role in determining the cannabinergic potency of tricyclic classical cannabinoids. We have synthesized a series of…”
Get full text
Journal Article -
20
Gas Phase and Solution Structures of 1-Methoxyallenyllithium
Published in Journal of organic chemistry (21-08-2009)“…A combined computational and 13C NMR study was used to determine the solution structures of 1-methoxyallenyllithium. The gas phase calculations indicated that…”
Get full text
Journal Article