Direct Alkylation of 1-Azabicyclo[1.1.0]butanes
Autor: | Ryan Gianatassio, Dora Kadish |
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Rok vydání: | 2019 |
Předmět: |
chemistry.chemical_classification
General method 010405 organic chemistry organic chemicals Organic Chemistry Butane Alkylation 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences Catalysis chemistry.chemical_compound chemistry Yield (chemistry) Reagent Organic chemistry Physical and Theoretical Chemistry Alkyl |
Zdroj: | Organic Letters. 21:2060-2063 |
ISSN: | 1523-7052 1523-7060 |
DOI: | 10.1021/acs.orglett.9b00321 |
Popis: | The facile synthesis of functionalized azetidines has been an ongoing challenge. Here, we report a general method to directly alkylate 1-azabicyclo[1.1.0]butane (ABB) with organometal reagents in the presence of Cu(OTf)2 to rapidly prepare bis-functionalized azetidines. This method allows for the preparation of azetidines bearing alkyl, allyl, vinyl, and benzyl groups. This catalyst system was extended to aziridines and spirocycles. Several building blocks and drug-like compounds were prepared in rapid fashion and in good yield. |
Databáze: | OpenAIRE |
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