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2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from November 2021
22 November 2021 Press Releases
Kyiv, Ukraine, 22 November 2021. Recently, Prof. Magolan and coworkers from McMaster University (Hamilton, Ontario, Canada) reported that hexafluoroisopropyl sulfamate (HFIPS) is a convenient reagent for the sulfamoylation of alcohols and amines (Org. Lett. 2021, 23, 3373–3378). HFIPS has also been used for metal-catalyzed C–H aminations (J. Am. Chem. Soc. 2014, 136, 5783–5789) and for the synthesis of aziridines using silver catalysis (Synthesis 2018, 50, 4462–4470) or electrochemical conditions (Angew. Chem. Int. Ed. 2018, 57, 5695–5698). Enamine has adapted and scaled-up the published procedure to synthesize HFIPS and make it more accessible to scientists worldwide. The reagent is now available in Enamine’s catalogue in multigram quantities.
Iryna Iavniuk, Business Development Director at Enamine, comments: “We at Enamine are committed to making novel reagents immediately accessible to our customers. We have successfully applied the HFIPS reagent in one of our projects previously and were happy to produce it for commercialization.”
Prof. Dr. Oleksandr Grygorenko, Consulting Scientist at Enamine, explains: “Dr. Jarrod Johnson, a Research Associate in the Magolan group, contacted us to point out that there was a supply gap with HFIPS. We recognized the usefulness of the reagent and happily agreed to begin commercialization. Our chemists quickly reproduced the published procedure to synthesize 50 grams of the reagent and HFIPS is now available from EnamineStore: https://www.enaminestore.com/catalog/EN300-1987789.”
Dr. Jarrod Johnson from McMaster University, adds: “We like the ease and simplicity of using HFIPS for sulfamoylation chemistry and hope it might become the go-to reagent for medicinal chemists making sulfamates and sulfamides.”
Prof. Dr. Jakob Magolan from McMaster University, comments: “It’s great to see Enamine now offering bulk HFIPS. I expect that this will enable creative scientists around the world to further extend the scope and applicability of this useful little reagent.”
Conflict of interest statement: Hereby the parties confirm that Prof. Magolan and his group have no financial interest in commercialization of EN300-1987789. No specialized data was transferred to Enamine apart from that already published in the literature.
18 October 2021 Press Releases
Kyiv, Ukraine, 18 October 2021. Several months ago, Prof. Levin and co-workers from University of Chicago developed an elegant method for the “skeletal editing” of organic molecules by nitrogen atom deletion (see Nature 2021, 593, 223–227). Their strategy included the use of an anomeric N-pivaloyloxy-N-alkoxyamide amide as the key reagent. Enamine, the world-leading compound supplier, is proud to announce that this reagent has been just added to the company’s product catalog. The compound is now available from the company’s stock in multigram quantities.
Iryna Iavniuk, Business Development Director at Enamine, explains: “We at Enamine always look for the most recent scientific findings in all areas of chemistry and use them to expand and improve our products immediately. We were happy to collaborate with Mark Levin on the commercialization of his fascinating reagent – a remarkable addition to our reagent collection.”
Prof. Dr. Oleksandr Grygorenko, Consulting Scientist at Enamine, adds: “I was really excited when I saw Prof. Levin’s Nature publication on the nitrogen deletion method while surfing the literature. When Mark contacted us, we readily agreed to collaborate. Our chemists quickly reproduced his published protocols, performed scale-up to 50 g of the reagent, demonstrated its applicability, and checked the storage stability. Now, the compound is available from EnamineStore: https://www.enaminestore.com/catalog/EN300-33050767“
Prof. Dr. Mark Levin, Assistant Professor at University of Chicago, comments: “Hopefully anyone who wants to give our methods a whirl will be able to take advantage of this wonderful offering from Enamine. I am looking forward to all the creative applications of nitrogen deletion that this will enable!”
Conflict of interest statement: Hereby the parties confirm that Prof. Levin or his group has no financial interest in commercialization of EN300-33050767. No specialized data was transferred to Enamine apart from that already published in the literature.
15 October 2021 News
A group of scientists led by Qubit cooperated on computer-driven de novo design of potential active molecules, with the subsequent synthesis of the most promising inhibitors by Enamine and their in vitro activity testing at Università degli Studi di Padova.