Diversity-orientated synthesis of macrocyclic heterocycles using a double SAr approach
An efficient macrocyclisation approach based on the double aromatic nucleophilic substitution (SNACK) was developed. This methodology allows a facile incorporation of heterocyclic motifs into macrocyclic rings and rapid synthesis of a significant number of structurally diverse macrocycles. SNACK mac...
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| Veröffentlicht in: | Organic & biomolecular chemistry 2021-07, Vol.19 (28), p.6274-629 |
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| container_issue | 28 |
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| container_title | Organic & biomolecular chemistry |
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| creator | Raubo, Piotr Carbajo, Rodrigo J McCoull, William Raubo, Joanna Thomas, Morgan |
| description | An efficient macrocyclisation approach based on the double aromatic nucleophilic substitution (SNACK) was developed. This methodology allows a facile incorporation of heterocyclic motifs into macrocyclic rings and rapid synthesis of a significant number of structurally diverse macrocycles. SNACK macrocyclisation enables preparation of stable diastereoisomers of conformationally restricted macrocycles (atropisomers). Practical application of SNACK macrocyclisation in a drug discovery project was exemplified by the identification of high affinity macrocyclic binders of B-cell lymphoma 6 (BCL6).
An efficient macrocyclisation approach based on the double aromatic nucleophilic substitution (SNACK) was developed. |
| doi_str_mv | 10.1039/d1ob00612f |
| format | Article |
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| ispartof | Organic & biomolecular chemistry, 2021-07, Vol.19 (28), p.6274-629 |
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| source | Royal Society Of Chemistry Journals; Alma/SFX Local Collection |
| title | Diversity-orientated synthesis of macrocyclic heterocycles using a double SAr approach |
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