Building Complexity and Achieving Selectivity through Catalysis - Case Studies from the Pharmaceutical Pipeline

被引：10

作者：

Beaver, Matthew G. ^{[1
]}

Caille, Seb ^{[2
]}

Farrell, Robert P. ^{[2
]}

Roetheli, Andreas R. ^{[1
]}

Smith, Austin G. ^{[2
]}

Tedrow, Jason S. ^{[1
]}

Thiel, Oliver R. ^{[1
]}

机构：

[1] Amgen Inc, Drug Subst Technol, Proc Dev, 360 Binney St, Cambridge, MA 02142 USA

[2] Amgen Inc, Drug Subst Technol, Proc Dev, One Amgen Ctr Dr, Thousand Oaks, CA 91320 USA

来源：

SYNLETT | 2021年 / 32卷 / 05期

关键词：

catalysis; process development; drug development; green chemistry; synthetic methods;

D O I：

10.1055/s-0040-1706869

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

http://www.w3.org/1999/xlink Abstract The last decade of small-molecule process development has witnessed a trend of increasing molecular complexity for clinical candidates. The continued advance of novel catalytic methods and subsequent translation to efficient and scalable processes has enabled process chemists to overcome the challenges associated with increasing complexity. This Account highlights several examples from the process chemistry laboratories at Amgen. 1 Introduction 2 The Evolution of Molecular Complexity 3 Catalysis as a Lever to Build Complexity 4 Ru(II)-Catalyzed Dynamic Kinetic Resolution Enabling the Manufacture of AMG 232 5 Application of Enzymatic Desymmetrization toward Scale-Up of the MCL-1 Inhibitor AMG 176 6 Synthesis of Fucostatin 1: Catalytic Asymmetric Transfer Hydrogenation 7 Manganese-Catalyzed Asymmetric Epoxidation To Prepare a Carfilzomib Intermediate 8 Asymmetric Reduction Strategies: Novel Apelin Receptor Agonists and AMG 986 9 Conclusions

引用

页码：457 / 471

页数：15

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