Table of Contents:
  • Synthesis of a Potent NAE Inhibitor: Pevonedistat / Mizutani, Hirotaki; Langston, Steven; Vyskocil, Stepan / http://dx.doi.org/10.1021/bk-2016-1240.ch001
  • Process Development and GMP Production of a Potent NEDD8-Activating Enzyme (NAE) Inhibitor: Pevonedistat / Armitage, Ian; McCarron, Ashley; Zhu, Lei / http://dx.doi.org/10.1021/bk-2016-1240.ch002
  • The Discovery and Synthesis of the CGRP Receptor Antagonist MK-3207 / Bell, Ian M., Department of Discovery Chemistry, Merck and Company, Incorporated, 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States; Bulger, Paul G., Department of Process Research and Development, Merck and Company, Incorporated, 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States; McLaughlin, Mark, Department of Process Research and Development, Merck and Company, Incorporated, 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States / http://dx.doi.org/10.1021/bk-2016-1240.ch003
  • Design and Enabling Development of Hydroxyethylamine-Derived BACE1 Inhibitor / Tedrow, Jason S., Process Development, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States; Zhong, Wenge, Discovery Research, Amgen Asia R&D Center, 99 Haike Road, 4th Floor, Building 6, Shanghai 201210, P. R. China / http://dx.doi.org/10.1021/bk-2016-1240.ch004
  • Identification and Optimization of a Series of Non-Steroidal Trifluoromethylcarbinol Glucocorticoid Receptor Agonists / Harcken, Christian, Department of Immunology and Respiratory Discovery Research, Boehringer Ingelheim Pharmaceuticals, Incorporated, 900 Ridgebury Road, Ridgefield, Connecticut 06778, United States; Razavi, Hossein, Department of Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Incorporated, 900 Ridgebury Road, Ridgefield, Connecticut 06778, United States / http://dx.doi.org/10.1021/bk-2016-1240.ch005
  • Development of an Asymmetric Route for Large-Scale Synthesis of a Glucocorticoid Agonist / Reeves, Jonathan T.; Fandrick, Daniel R.; Song, Jinhua J.; Tan, Zhulin; Kim, Soojin; Yang, Bing-Shiou; Yee, Nathan K.; Senanayake, Chris H. / http://dx.doi.org/10.1021/bk-2016-1240.ch006
  • The Medicinal Chemistry and Commercial Manufacturing Behind the Discovery and Development of the Hedgehog Inhibitor Vismodegib / Angelaud, Remy, Small Molecule Process Chemistry, Genentech, A Member of the Roche Group, 1 DNA Way, South San Francisco, California 94080, United States; Sutherlin, Daniel P., Discovery Chemistry, Genentech, A Member of the Roche Group, 1 DNA Way, South San Francisco, California 94080, United States; Reynolds, Mark, Small Molecule Process Chemistry, Genentech, A Member of the Roche Group, 1 DNA Way, South San Francisco, California 94080, United States; Savage, Scott, Small Molecule Process Chemistry, Genentech, A Member of the Roche Group, 1 DNA Way, South San Francisco, California 94080, United States; Stumpf, Andreas, Small Molecule Process Chemistry, Genentech, A Member of the Roche Group, 1 DNA Way, South San Francisco, California 94080, United States / http://dx.doi.org/10.1021/bk-2016-1240.ch007
  • Discovery and Process Development of Class I PI3K and Class I PI3K/mTOR Inhibitors GDC-0941 and GDC-0980 / Babu, Srinivasan, Small Molecule Process Chemistry, Genentech, Incorporated, 1 DNA Way, South San Francisco, California 94080, United States; Gosselin, Francis, Small Molecule Process Chemistry, Genentech, Incorporated, 1 DNA Way, South San Francisco, California 94080, United States; Humphries, Theresa, Small Molecule Process Chemistry, Genentech, Incorporated, 1 DNA Way, South San Francisco, California 94080, United States; Olivero, Alan, Discovery Chemistry, Genentech, Incorporated, 1 DNA Way, South San Francisco, California 94080, United States; Sutherlin, Daniel, Discovery Chemistry, Genentech, Incorporated, 1 DNA Way, South San Francisco, California 94080, United States; Tian, Qingping, Small Molecule Process Chemistry, Genentech, Incorporated, 1 DNA Way, South San Francisco, California 94080, United States / http://dx.doi.org/10.1021/bk-2016-1240.ch008
  • The Development and Manufacture of Azacitidine, Decitabine, and Cladribine: Stereoselective Ribonucleoside Drug Synthesis Using the Vorbrüggen Glycosylation / Co, Erick W.; Henschke, Julian P. / http://dx.doi.org/10.1021/bk-2016-1240.ch009
  • Editors’ Biographies / http://dx.doi.org/10.1021/bk-2016-1240.ot001