HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Hydrochloric Acid → Hydrochloric Acid
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Hydrochloric Acid | HCID 313 | — |
| Edukt | Paclitaxel | HCID 36314 | — |
| Edukt | N-Benzoyl-3-phenylisoserine, (2R,3S)- | HCID 2762289 | — |
| Produkt | Hydrochloric Acid | HCID 313 | — |
| Produkt | 3-Phenylisoserine, (2R,3S)- | HCID 7020763 | — |
Reaktionsschritte
When the desired product is the side chain of taxol, N-benzoyl-(2R,3S)-3-phenylisoserine, R1 is phenyl, and R7 is preferably trimethylsilyl. In this synthesis the product of the reaction Scheme 1 is (3R,4S)-3-triisopropylsilyloxy-4-phenyl-2-azetidin-2-one (see Scheme 2), which is hydrolyzed, for example with hydrochloric acid, to yield the corresponding (2R,3S)-3-phenylisoserine as hydrochloric acid salt. The phenylisoserine is then benzoylated by procedures known in the art, for example, the Schotten-Baumann procedure, and purified, if necessary, by recrystallization or through a short silica gel column to give enantiomerically pure N-benzoyl-(2R,3S)-3-phenylisoserine (see Scheme 3).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US05294737 |
| Quelldatensatz | uspto-grants-1994_03 |
| ORD ID | ord-05c00a002a324716adc70b5184b49e02 |
| Quellennotiz | uspto-grants-1994_03 |