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Full Description
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.
Contents
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
