Full Text Journal Articles by
Author Stefan G Koenig


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Introduction of a process mass intensity metric for biologics.

Kristi Budzinski, Megan Blewis, Philip Dahlin, Daniel D'Aquila, Julia Esparza, Jack Gavin, Sa V Ho, Clarice Hutchens, David Kahn, Stefan G Koenig, Robert Kottmeier, Jeff Millard, Matt Snyder, Brad Stanard, Lixin Sun,

Biopharmaceuticals (or biologics), large molecule therapeutics typically produced using biotechnology, are a rapidly growing segment of the pharmaceutical market. As such, the environmental footprint of the production of these molecules is coming under scrutiny from various stakeholders such as healthcare providers, investors, and even employees. Process mass intensity (PMI), originally ... Read more >>

N Biotechnol (New biotechnology)
[2019, 49:37-42]

Cited: 1 time

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GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).

F Anthony Romero, Jeremy Murray, Kwong Wah Lai, Vickie Tsui, Brian K Albrecht, Le An, Maureen H Beresini, Gladys de Leon Boenig, Sarah M Bronner, Emily W Chan, Kevin X Chen, Zhongguo Chen, Edna F Choo, Kyle Clagg, Kevin Clark, Terry D Crawford, Patrick Cyr, Denise de Almeida Nagata, Karen E Gascoigne, Jane L Grogan, Georgia Hatzivassiliou, Wei Huang, Thomas L Hunsaker, Susan Kaufman, Stefan G Koenig, Ruina Li, Yingjie Li, Xiaorong Liang, Jiangpeng Liao, Wenfeng Liu, Justin Ly, Jonathan Maher, Colin Masui, Mark Merchant, Yingqing Ran, Alexander M Taylor, John Wai, Fei Wang, Xiaocang Wei, Dong Yu, Bing-Yan Zhu, Xiaoyu Zhu, Steven Magnuson,

Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderately potent and selective over BRD4(1). In pursuit of a more potent and selective CBP inhibitor, ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2017, 60(22):9162-9183]

Cited: 8 times

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Highly Efficient Synthesis of a Staphylococcus aureus Targeting Payload to Enable the First Antibody-Antibiotic Conjugate.

Xin Linghu, Nathaniel L Segraves, Ifat Abramovich, Nicholas Wong, Barbara Müller, Nadja Neubauer, Serena Fantasia, Sebastian Rieth, Stephan Bachmann, Michael Jansen, C Gregory Sowell, David Askin, Stefan G Koenig, Francis Gosselin,

A practical synthesis of the complex payload for an anti-Staphylococcus aureus THIOMABTM antibody-antibiotic conjugate (TAC) is described. The route takes advantage of a delicate oxidative condensation, achieved using a semi-continuous flow procedure. It allows for the generation of kilogram quantities of a key intermediate to enable a mild nucleophilic aromatic ... Read more >>

Chemistry (Chemistry (Weinheim an der Bergstrasse, Germany))
[2018, 24(12):2837-2840]

Cited: 2 times

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A call for industry to embrace green biopharma.

Kristi L Budzinski, Stefan G Koenig, Deborah A O'Connor, Tse-Sung Wu,

Nat. Biotechnol. (Nature biotechnology)
[2016, 34(3):234-235]

Cited: 0 times

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Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody-drug conjugates.

Leanna R Staben, Stefan G Koenig, Sophie M Lehar, Richard Vandlen, Donglu Zhang, Josefa Chuh, Shang-Fan Yu, Carl Ng, Jun Guo, Yanzhou Liu, Aimee Fourie-O'Donohue, MaryAnn Go, Xin Linghu, Nathaniel L Segraves, Tao Wang, Jinhua Chen, BinQing Wei, Gail D Lewis Phillips, Keyang Xu, Katherine R Kozak, Sanjeev Mariathasan, John A Flygare, Thomas H Pillow,

The reversible attachment of a small-molecule drug to a carrier for targeted delivery can improve pharmacokinetics and the therapeutic index. Previous studies have reported the delivery of molecules that contain primary and secondary amines via an amide or carbamate bond; however, the ability to employ tertiary-amine-containing bioactive molecules has been ... Read more >>

Nat Chem (Nature chemistry)
[2016, 8(12):1112-1119]

Cited: 23 times

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Synthesis of Indole-2-carboxylate Derivatives via Palladium-Catalyzed Aerobic Amination of Aryl C-H Bonds.

Kyle Clagg, Haiyun Hou, Adam B Weinstein, David Russell, Shannon S Stahl, Stefan G Koenig,

A direct oxidative C-H amination affording 1-acetyl indolecarboxylates starting from 2-acetamido-3-arylacrylates has been achieved. Indole-2-carboxylates can be targeted with a straightforward deacetylation of the initial reaction products. The C-H amination reaction is carried out using a catalytic Pd(II) source with oxygen as the terminal oxidant. The scope and application of ... Read more >>

Org. Lett. (Organic letters)
[2016, 18(15):3586-3589]

Cited: 4 times

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Chemoselective sp2-sp3 cross-couplings: iron-catalyzed alkyl transfer to dihaloaromatics.

Sushant Malhotra, Pamela S Seng, Stefan G Koenig, Alan J Deese, Kevin A Ford,

The chemoselective functionalization of a range of dihaloaromatics with methyl, cyclopropyl, and higher alkyl Grignard reagents via iron-catalyzed cross-coupling is described. The site selectivity of C-X (X = halogen) activation is determined by factors such as the position of the halogen on the ring, the solvent, and the nucleophile. A ... Read more >>

Org. Lett. (Organic letters)
[2013, 15(14):3698-3701]

Cited: 7 times

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A facile deprotection of secondary acetamides.

Stefan G Koenig, Charles P Vandenbossche, Hang Zhao, Patrick Mousaw, Surendra P Singh, Roger P Bakale,

Imidoyl chlorides, generated from secondary acetamides and oxalyl chloride, can be harnessed for a selective and practical deprotection sequence. Treatment of these intermediates with 2 equiv of propylene glycol and warming enables the rapid release of amine hydrochloride salts in good yields. Notably, the reaction conditions are mild enough to ... Read more >>

Org. Lett. (Organic letters)
[2009, 11(2):433-436]

Cited: 5 times

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An efficient synthesis of enamides from ketones.

Hang Zhao, Charles P Vandenbossche, Stefan G Koenig, Surendra P Singh, Roger P Bakale,

A new synthesis of enamides from ketones is disclosed that involves a phosphine-mediated reductive acylation of oximes. The resulting enamides are isolated in good yields (up to 89%) and excellent purity, permitting a subsequent hydrogenation to access enantiopure acetamides at catalyst loadings practical for large-scale applications. ... Read more >>

Org. Lett. (Organic letters)
[2008, 10(3):505-507]

Cited: 7 times

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A transient N-O-linked Pauson-Khand strategy for the synthesis of the deschloro carbocyclic core of the palau'amines and styloguanidines.

Stefan G Koenig, Stefan M Miller, Kristi A Leonard, Ralf S Löwe, Betty C Chen, David J Austin,

A stereocontrolled route to the deschloro cyclopentyl core of the palau'amines and styloguanidines has been developed. This strategy makes use of the intramolecular Pauson-Khand cyclization of an enyne with a "transient N-O tether" to construct a five-membered carbocycle in a diastereoselective fashion. [reaction: see text] ... Read more >>

Org. Lett. (Organic letters)
[2003, 5(13):2203-2206]

Cited: 20 times

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