Fluorine in medicinal chemistry

HJ Böhm, D Banner, S Bendels, M Kansy… - …, 2004 - Wiley Online Library
Fluorinated compounds are synthesized in pharmaceutical research on a routine basis and
many marketed compounds contain fluorine. The present review summarizes some of the …

Trifluoromethylation of aryl and heteroaryl halides

S Roy, BT Gregg, GW Gribble, VD Le, S Roy - Tetrahedron, 2011 - Elsevier
The trifluoromethyl group (CF3) is an important structural moiety present in diverse classes
of bioactive organic molecules including novel pharmaceuticals and agrochemicals. 1 e4 In …

The role of fluorine in glycomimetic drug design

R Hevey - Chemistry–A European Journal, 2021 - Wiley Online Library
Glycans are well established to play important roles at various stages of infection and
disease, and ways to modulate these interactions have been sought as novel therapies. The …

[图书][B] Medicinal chemistry: a molecular and biochemical approach

T Nogrady, DF Weaver - 2005 - books.google.com
Fully updated and rewritten by a basic scientist who is also a practicing physician, the third
edition of this popular textbook remains comprehensive, authoritative and readable. Taking …

Substance P: structure, function, and therapeutics

P Datar, S Srivastava, E Coutinho… - Current topics in …, 2004 - ingentaconnect.com
Extensive efforts since 1931, on the structural determination of the mammalian tachykinin SP
by NMR, CD and IR have turned out to be inconclusive. Studies are now being concentrated …

Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced Diastereoselective Transformation

KMJ Brands, JF Payack, JD Rosen… - Journal of the …, 2003 - ACS Publications
An efficient stereoselective synthesis of the orally active NK1 receptor antagonist Aprepitant
is described. A direct condensation of N-benzyl ethanolamine with glyoxylic acid yielded a 2 …

Transition-Metal-Free N–O Reduction of Oximes: A Modular Synthesis of Fluorinated Pyridines

H Huang, J Cai, H Xie, J Tan, F Li, GJ Deng - Organic letters, 2017 - ACS Publications
An NH4I-based reductive system has been explored to promote the oxime N–O bond
cleavage and thereby enable a modular synthesis of a broad range of pharmacologically …

Utilization of an Intramolecular Hydrogen Bond To Increase the CNS Penetration of an NK1 Receptor Antagonist

VA Ashwood, MJ Field, DC Horwell… - Journal of medicinal …, 2001 - ACS Publications
This paper describes the synthesis and physical and biological effects of introducing
different substituents at the α-position of the tryptophan containing neurokinin-1 receptor …

Synthesis of trifluoromethylated and gem-difluoromethylenated biologically interesting compounds from fluorine-containing synthons

FL Qing, F Zheng - Synlett, 2011 - thieme-connect.com
A number of fluorinated versatile building blocks (synthons) were developed for the
synthesis of trifluoromethylated and gem-difluoromethylenated biologically interesting …

Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK1/NK2 Receptor Antagonist Activity

JS Albert, D Aharony, D Andisik… - Journal of medicinal …, 2002 - ACS Publications
Through optimization of compounds based on the dual NK1/NK2 antagonist ZD6021, it was
found that alteration of two key regions could modulate the balance of NK1 and NK2 …