On the design of complex drug candidate syntheses in the pharmaceutical industry

A data-driven strategy for predicting greenness scores, rationally comparing synthetic routes and benchmarking PMI outcomes for the synthesis of molecules in the pharmaceutical industry

(2017) Jun Li et al.   GREEN CHEMISTRY

Case Studies Illustrating a Science and Risk-Based Approach to Ensuring Drug Quality When Using Enzymes in the Manufacture of Active Pharmaceuticals Ingredients for Oral Dosage Form

(2016) Andrew S. Wells et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Scalable Synthesis of the Potent HIV Inhibitor BMS-986001 by Non-Enzymatic Dynamic Kinetic Asymmetric Transformation (DYKAT)

(2015) Adrian Ortiz et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Development of an Asymmetric Synthesis of a Chiral Quaternary FLAP Inhibitor

(2015) Keith R. Fandrick et al.   JOURNAL OF ORGANIC CHEMISTRY

Development of a Diastereoselective Phosphorylation of a Complex Nucleoside via Dynamic Kinetic Resolution

(2015) Kristy Tran et al.   JOURNAL OF ORGANIC CHEMISTRY

Ni-Catalyzed C–H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543

(2015) Monica A Fitzgerald et al.   JOURNAL OF ORGANIC CHEMISTRY

Mechanistic Insights into the Vanadium-Catalyzed Achmatowicz Rearrangement of Furfurol

(2015) Yining Ji et al.   JOURNAL OF ORGANIC CHEMISTRY

Current complexity: a tool for assessing the complexity of organic molecules

(2015) Jun Li et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Development of a Two-Step, Enantioselective Synthesis of an Amino Alcohol Drug Candidate

(2015) Michael A. Schmidt et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Preparation of β-hydroxy-α-amino Acid Using Recombinant d-Threonine Aldolase

(2015) Steven L. Goldberg et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Remarkable Enhancement of Enantioselectivity in the Asymmetric Conjugate Addition of Dimethylzinc to (Z)-Nitroalkenes with a Catalytic [(MeCN)4Cu]PF6-Hoveyda Ligand Complex

(2014) Xingzhong Zeng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis of the 6-Azaindole Containing HIV-1 Attachment Inhibitor Pro-Drug, BMS-663068

(2014) Ke Chen et al.   JOURNAL OF ORGANIC CHEMISTRY

All-Carbon Quaternary Stereogenic Centers in Acyclic Systems through the Creation of Several C–C Bonds per Chemical Step

(2014) Ilan Marek et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of a Concise, Asymmetric Synthesis of a Smoothened Receptor (SMO) Inhibitor: Enzymatic Transamination of a 4-Piperidinone with Dynamic Kinetic Resolution

(2014) Zhihui Peng et al.   ORGANIC LETTERS

A Claisen Approach to 4′-Ed4T

(2014) William P. Gallagher et al.   ORGANIC LETTERS

Addressing the Configuration Stability of Lithiated Secondary Benzylic Carbamates for the Development of a Noncryogenic Stereospecific Boronate Rearrangement

(2014) Keith R. Fandrick et al.   ORGANIC LETTERS

A Method for Heteroaromatic Nitration Demonstrating Remarkable Thermal Stability

(2014) Gregory L. Beutner et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Development of a Robust Process for the Preparation of High-Quality Dicyclopropylamine Hydrochloride

(2014) Boguslaw Mudryk et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Regioselective Bromination of Fused Heterocyclic N-Oxides

(2013) Sarah E. Wengryniuk et al.   ORGANIC LETTERS

Process Development of Halaven®: Synthesis of the C14-C35 Fragment via Iterative Nozaki-Hiyama-Kishi Reaction-Williamson Ether Cyclization

(2013) Charles Chase et al.   SYNLETT

Commercial Manufacture of Halaven®: Chemoselective Transformations En Route to Structurally Complex Macrocyclic Ketones

(2013) Francis Fang et al.   SYNLETT

Use of Enzymes in the Manufacture of Active Pharmaceutical Ingredients—A Science and Safety-Based Approach To Ensure Patient Safety and Drug Quality

(2012) Andrew S. Wells et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Enantioselective Construction of Quaternary Stereogenic Centers from Tertiary Boronic Esters: Methodology and Applications

(2011) Ravindra P. Sonawane et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Highly Enantioselective Synthesis of Tertiary Boronic Esters and their Stereospecific Conversion to other Functional Groups and Quaternary Stereocentres

(2011) Helen K. Scott et al.   CHEMISTRY-A EUROPEAN JOURNAL

Regioselective synthesis of 1,4-disubstituted imidazoles

(2011) Michael A. Schmidt et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

The Development of Scalable and Efficient Methods for the Preparation of Dicyclopropylamine HCl Salt

(2011) Ke Chen et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened

(2011) Michael J. Munchhof et al.   ACS Medicinal Chemistry Letters

Full Chirality Transfer in the Conversion of Secondary Alcohols into Tertiary Boronic Esters and Alcohols Using Lithiation-Borylation Reactions

(2010) Viktor Bagutski et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Development of a Dynamic Kinetic Resolution for the Isolation of an Intermediate in the Synthesis of Casopitant Mesylate: Application of QbD Principles in the Definition of the Parameter Ranges, Issues in the Scale-Up and Mitigation Strategies

(2010) Fernando Bravo et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Biocatalytic Asymmetric Synthesis of Chiral Amines from Ketones Applied to Sitagliptin Manufacture

(2010) C. K. Savile et al.   SCIENCE

Improved method for the conversion of pinacolboronic esters into trifluoroborate salts: facile synthesis of chiral secondary and tertiary trifluoroborates

(2009) Viktor Bagutski et al.   TETRAHEDRON

Enantiodivergent conversion of chiral secondary alcohols into tertiary alcohols

(2008) Jake L. Stymiest et al.   NATURE