Guo-Qiang Lin & Qi-Dong You 
Chiral Drugs [EPUB ebook] 
Chemistry and Biological Action

An integrated view of chiral drugs–from concept and
synthesisto pharmaceutical properties

Chirality greatly influences a drug’s biological and
pharmacological properties. In an effort to achieve more
predictable results from chiral drugs, the Food and Drug
Administration now requires that these medicines be as pure as
possible, which places great demands on drug synthesis,
purification, analysis, and testing. To assist researchers in
acquiring the essential knowledge to meet these rigid guidelines,
Chiral Drugs focuses on three vital chiral
technologies–asymmetric synthesis, biocatalytic process, and
chiral resolution–to offer details on the basic concepts, key
developments, and recent trends in chiral drug discovery, along
with:

* The history of chiral drugs development and industrial
applications of chiral technologies

* A section listing twenty-five approved or advanced-trial chiral
drugs that lists each drug name, chemical name and properties, a
representative synthetic pathway, pharmacological
characterizations, and references

* An interdisciplinary approach combining synthetic organic
chemistry, medicinal chemistry, and pharmacology

Nearly two-thirds of the drugs on today’s market are chiral
drugs. Reducing and eliminating their negative characteristics is
an ongoing and serious challenge for the pharmaceutical industry.
With its well-balanced approach to covering each important aspect
of chirality, Chiral Drugs champions important strategies for
tipping the medical scale in a positive direction for the
production of more effective–and safer–drugs.

Daftar Isi

ABOUT THE EDITORS vii

CONTRIBUTORS ix

INTRODUCTION 1

1 OVERVIEW OF CHIRALITY AND CHIRAL DRUGS 3

Guo-Qiang Lin, Jian-Ge Zhang, and Jie-Fei Cheng

2 CHIRAL DRUGS THROUGH ASYMMETRIC SYNTHESIS 29

Guo-Qiang Lin and Xing-Wen Sun

3 CHIRAL DRUGS VIA BIOCATALYTICAL APPROACHES 77

Jianqiang Wang and Wenya Lu

4 RESOLUTION OF CHIRAL DRUGS 137

Qi-Dong You

5 FLUORINE-CONTAINING CHIRAL DRUGS 195

Xiao-Long Qiu, Xuyi Yue, and Feng-Ling Qing

6 INDUSTRIAL APPLICATION OF CHIRAL TECHNOLOGIES 253

Hui-Yin (Harry) Li, Rui Liu, Carl Behrens, and Chao-Ying
Ni

7 STRUCTURAL BASIS AND COMPUTATIONAL MODELING OF CHIRAL DRUGS
297

Deping Wang and Eric Hu

8 PHARMACOLOGY OF CHIRAL DRUGS 323

Yongge Liu and Xiao-Hui Gu

9 PHARMACOKINETICS OF CHIRAL DRUGS 347

Hanqing Dong, Xiaochuan Guo and Zengbiao Li

10 TOXICOLOGY OF CHIRAL DRUGS 381

Guang Yang and Hai-Zhi Bu

11 REPRESENTATIVE CHIRAL DRUGS 401

Jiangqin Sun, Dingguo Liu, and Zhimin Wang

INDEX 449

Tentang Penulis

GUO-QIANG LIN, is a professor at the Shanghai Institute of
Organic Chemistry and an adjunct professor at Fudan University,
China. He is the Director of the Division of Chemical Science of
the National Natural Science Foundation of China. Among Professor
Lin’s publications are the Wiley books Principles and Applications
of Asymmetric Synthesis and Biocatalysis for the Pharmaceutical
Industry.

QI-DONG YOU, PHD, is the Dean and a professor of the
School of Pharmacy at China Pharmaceutical University. He is an
Associate Editor of Progress in Pharmaceutical Sciences and serves
on the Editorial Board of the International Journal of Medicinal
Chemistry and Acta Pharmaceutica Sinica. Dr. You is a coauthor of
over eighty publications, and an inventor or co-inventor of over
twenty patent applications and patents.

JIE-FEI CHENG, PHD, is the Director of Otsuka Shanghai Research
Institute, a fully owned subsidiary of Otsuka Pharmaceutical Co.,
Ltd Japan. Formerly an associate professor at Shanghai Institute of
Organic Chemistry, he has worked for over fifteen years in the
pharmaceutical and biotech industries in the United States. Dr.
Cheng is a coauthor of over fifty peer-reviewed publications, and
an inventor or coinventor of over twenty patent applications and
patents.