A convenient and versatile S N Ar-decarboxylation protocol for the construction of C(sp 2 )-C(sp 3 ) bonds.
| Autor: | Burtea A; Oncology Medicinal Chemistry, Pfizer Worldwide Research, Development and Medical, 10770 Science Center Drive, San Diego, CA 92121, USA. Gary.Gallego@pfizer.com., DeForest J; Oncology Medicinal Chemistry, Pfizer Worldwide Research, Development and Medical, 10770 Science Center Drive, San Diego, CA 92121, USA. Gary.Gallego@pfizer.com., Baldwin N; Pfizer Medicine Design, 445 Eastern Point Rd, Groton, CT 06340, USA., Leverett C; Pfizer Medicine Design, 445 Eastern Point Rd, Groton, CT 06340, USA., Gallego GM; Oncology Medicinal Chemistry, Pfizer Worldwide Research, Development and Medical, 10770 Science Center Drive, San Diego, CA 92121, USA. Gary.Gallego@pfizer.com. |
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| Jazyk: | angličtina |
| Zdroj: | Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2022 Jun 30; Vol. 58 (53), pp. 7435-7438. Date of Electronic Publication: 2022 Jun 30. |
| DOI: | 10.1039/d2cc01551j |
| Abstrakt: | Increasing saturation (Fsp 3 ) remains a central strategy in the optimization of properties of molecules during drug discovery. Here, we describe a versatile and operationally simple one-pot procedure for accomplishing this goal via a nucleophilic aromatic substitution-decarboxylation sequence to construct C(sp 2 )-C(sp 3 ) bonds. The method is tolerant of a variety of biologically privileged moieties and has been demonstrated in a library format. |
| Databáze: | MEDLINE |
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