ABSTRACT

Drug Discovery with Privileged Building Blocks traces back PharmaBlock’s founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to biological activities of different molecules but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and a regular analysis of new building block structures in the latest researches have proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book.

Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists, and veteran medicinal chemists will find it useful as well.

Key Feature

  1. The book covers privileged building blocks appearing most frequently on patents for novel drugs.
  2. The latest relevant tactics are explained in the context of drug design and medicinal chemistry.
  3. Key synthesis, especially large-scale synthesis, is described.
  4. The most recent literature references are cited.

chapter 1|15 pages

Alkynes

chapter 2|11 pages

Azaindoles

chapter 3|4 pages

Azetidines

chapter 7|10 pages

Bicyclo[3.1.0]hexanes

chapter 9|9 pages

Cubanes, Are We There Yet?

chapter 10|7 pages

Cyclobutanes

chapter 11|13 pages

Cyclohexanes

chapter 12|6 pages

Cyclopentanes

chapter 14|4 pages

Deazapurines

chapter 15|8 pages

Furopyridines

chapter 16|13 pages

Indazoles

chapter 17|9 pages

Indoles

chapter 18|6 pages

Oxetanes

chapter 19|4 pages

Piperidine, the Enchanted Ring

chapter 20|10 pages

Pyrazines

chapter 21|13 pages

Pyrazoles

chapter 22|9 pages

Pyridazines

chapter 24|10 pages

Pyrimidines

chapter 25|14 pages

Pyrrolidines

chapter 26|9 pages

Pyrrolotriazines

chapter 27|8 pages

Spiroazetidines

chapter 28|7 pages

Spirocyclic Piperidines

chapter 29|9 pages

Spirocyclic Pyrrolidines

chapter 30|5 pages

Spirooxetanes

chapter 31|12 pages

Tetrahydropyrans

chapter 32|9 pages

Trifluoromethylpyridines