298693-79-5Relevant articles and documents
Synthesis of Enantiopure Unnatural Amino Acids by Metallaphotoredox Catalysis
Agejas, Javier,Barberis, Mario,De Frutos, Oscar,Faraggi, Tomer M.,García-Cerrada, Susana,MacMillan, David W. C.,Mateos, Carlos,Rincón, Juan A.,Rouget-Virbel, Caroline
supporting information, p. 1966 - 1973 (2021/08/18)
We describe herein a two-step process for the conversion of serine to a wide array of optically pure unnatural amino acids. This method utilizes a photocatalytic cross-electrophile coupling between a bromoalkyl intermediate and a diverse set of aryl halides to produce artificial analogues of phenylalanine, tryptophan, and histidine. The reaction is tolerant of a broad range of functionalities and can be leveraged toward the scalable synthesis of valuable pharmaceutical scaffolds via flow technology.
OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO
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Page/Page column 76, (2019/10/29)
Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R3, R4, R5, R6, R8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
Mild palladium-catalyzed cyanation of (hetero)aryl halides and triflates in aqueous media
Cohen, Daniel T.,Buchwald, Stephen L.
supporting information, p. 202 - 205 (2015/01/30)
A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.