Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Chlorosuccinimide | HCID 31398 | — |
| Edukt | 4-Bromo-3-fluorobenzoic acid | HCID 2773341 | — |
| Edukt | 1-(4-Bromo-2-chlorophenyl)ethan-1-one | HCID 15560950 | — |
| Edukt | 3-((R)-1-{(S)-1-[5-(4-iodo-phenyl)-1H-imidazol-2-yl]-2-methyl-propyl}-2,5-dioxo-imidazolidin-4-yl)-propionic acid | HCID 57771978 | — |
| Edukt | (R)-tert-butoxycarbonylamino-(4-dimethylcarbamoylmethoxy-phenyl)-acetic acid | HCID 66815126 | — |
| Edukt | {(1S,2S)-1-[5-(2-fluoro-phenyl)-1H-imidazol-2-yl]-2-phenyl-propyl}-carbamic acid tert-butyl ester | HCID 67001749 | — |
| Produkt | 1-(4-Bromo-3-fluorophenyl)propan-1-one | HCID 24212087 | — |
Reaktionsschritte
Prepared by the same method as described in example 1 except that (i) steps A, B and C were omitted; (ii) 1-(4-bromo-3-fluoro-phenyl)-propan-1-one was used in place of 1-(2-fluoro-4-iodo-phenyl)-ethanone in step 21-D; (iii) (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid was used in place of (2S,3S)-2-tert-butoxycarbonylamino-3-phenyl-butyric acid in step 21-E; and (iv) chlorination of the 5-position of the imidazole ring with N-chlorosuccinimide in step 21-F was omitted. 1-(4-Bromo-3-fluoro-phenyl)-propan-1-one was prepared as described in example 6 for the preparation of 1-(4-bromo-2-chloro-phenyl)-ethanone except that 4-bromo-3-fluorobenzoic acid was used in place of 4-bromo-2-chlorobenzoic acid in step 21-I. HR-MS: calcd for C28H24BrFN4O4 [M+H+] 579.1038. Found 579.1038.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patentnummer | US08063085B2 |
|---|
| Quelldatensatz | uspto-grants-2011_11 |
|---|
| ORD ID | ord-eef49124d92f4b308d774c2a9447ce57 |
|---|
| Quellennotiz | uspto-grants-2011_11 |
|---|
