Solid-phase synthesis of novel 14-membered macroycles for high throughput screening
US6228986A · kind A · utility
12Cited by
1References
5Claims
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Key dates
| Filing date | Apr 7, 1999 |
| Grant date | May 8, 2001 |
| Priority date | — |
| Expiry date | Apr 7, 2019 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/06078
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
The preparation of 14-membered macrocycles from a resin-bound orthogonally protected lysine residue is described. Reductive alkylation of the a-nitrogen followed by acylation with an Fmoc-aminoacid provides a protected dipeptide precursor. Removal of the Fmoc-group, acylation with a succinic anhydride, methyltrityl-group removal and macrocyclization provides the desired macrocycles, after TFA cleavage, in excellent yield and purity.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.