201609-29-2Relevant articles and documents
2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS
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Paragraph 0985-0988, (2021/04/17)
Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.
Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character
Campbell, Peter S.,Jamieson, Craig,Simpson, Iain,Watson, Allan J. B.
, p. 46 - 49 (2017/12/27)
The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.
Engaging nonaromatic, heterocyclic tosylates in reductive cross-coupling with aryl and heteroaryl bromides
Molander, Gary A.,Traister, Kaitlin M.,O'Neill, Brian T.
, p. 2907 - 2911 (2015/03/18)
A method has been developed for the introduction of nonaromatic heterocyclic structures onto aryl and heteroaryl bromides using alkyl tosylates in a reductive cross-coupling manifold. This protocol offers an improvement over previous methods by utilizing alkyl tosylate coupling partners that are bench-stable, crystalline solids that can be prepared from inexpensive, commercially available alcohols.