Metabolic and pharmaceutical aspects of fluorinated compounds

BM Johnson, YZ Shu, X Zhuo… - Journal of medicinal …, 2020 - ACS Publications
The applications of fluorine in drug design continue to expand, facilitated by an improved
understanding of its effects on physicochemical properties and the development of synthetic …

Redox‐neutral TEMPO catalysis: direct radical (hetero) aryl C− H Di‐and trifluoromethoxylation

JW Lee, S Lim, DN Maienshein, P Liu… - Angewandte …, 2020 - Wiley Online Library
Applications of TEMPO. catalysis for the development of redox‐neutral transformations are
rare. Reported here is the first TEMPO.‐catalyzed, redox‐neutral C− H di‐and …

[HTML][HTML] Nucleophilic trifluoromethoxylation of alkyl halides without silver

Y Li, Y Yang, J Xin, P Tang - Nature Communications, 2020 - nature.com
The biological properties of molecules containing the trifluoromethoxy group have made
these compounds important targets in pharmaceuticals and agrochemicals, yet their …

Facile Access to AgOCF3 and Its New Applications as a Reservoir for OCF2 for the Direct Synthesis of N−CF3, Aryl or Alkyl Carbamoyl Fluorides

A Turksoy, T Scattolin… - … A European Journal, 2020 - Wiley Online Library
The development of innovative fluorination strategies is greatly dependent also on the
availability, safety and practicability of available fluorinating reagents. We herein show a …

Recent advance in development and application of electrophilic difluoromethylating reagents

W Qin, J Chen, W Xiong, G Liu - Chinese Journal of Organic …, 2020 - sioc-journal.cn
In the past two decades, the development and application of bench-stable electrophilic
difluoromethylating reagents have attracted considerable attention. Consequently, some …

[HTML][HTML] Photocatalytic trifluoromethoxylation of arenes and heteroarenes in continuous-flow

AV Nyuchev, T Wan, B Cendón… - Beilstein Journal of …, 2020 - beilstein-journals.org
The first example of photocatalytic trifluoromethoxylation of arenes and heteroarenes under
continuous-flow conditions is described. Application of continuous-flow microreactor …

Synthesis, physico-chemical properties and microsomal stability of compounds bearing aliphatic trifluoromethoxy group

IG Logvinenko, Y Markushyna, IS Kondratov… - Journal of Fluorine …, 2020 - Elsevier
Abstract Effects of the trifluoromethoxy substituent on physico-chemical properties of
compounds, such as kinetic solubility, lipophilicity and microsomal clearance, was studied in …

Synthesis and use of trifluoromethylthiolated ketenimines

T Guérin, NV Pikun, R Morioka… - … A European Journal, 2020 - Wiley Online Library
The synthesis of trifluoromethylthiolated ketenimines is herein described. They are easily
synthesized from the corresponding α‐trifluoromethylthiolated oximes upon activation with …

Superelectrophilic Csp 3–H bond fluorination of aliphatic amines in superacid: the striking role of ammonium–carbenium dications

M Artault, N Mokhtari, T Cantin… - Chemical …, 2020 - pubs.rsc.org
The superacid-promoted electrophilic Csp3–H bond activation of aliphatic amines generates
superelectrophilic species that can be subsequently fluorinated. Demonstrated by low …

Functionalization of 2‐Trifluoromethyl‐1H‐pyrrole: A Convenient Entry into Advanced Fluorinated Building Blocks Including all Isomeric 2‐(Trifluoromethyl)prolines

VY Hys, OI Shevchuk, BV Vashchenko… - European Journal of …, 2020 - Wiley Online Library
The synthetic utility of 2‐trifluoromethyl‐1H‐pyrrole as a pharmaceutically relevant platform
was demonstrated by the preparation of mono‐and bifunctional C‐2 (5)‐or C‐3‐substituted …