HuagongsheHuagongshe Chemistry Print Report · For research reference only
Boron trifluoride etherate → Methyl N-[(benzyloxy)carbonyl]-O-{(1S)-2-[(tert-butoxycarbonyl) (cyclopropylmethyl)amino]-1-phenylethyl}-D-serinate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Boron trifluoride etherate | HCID 8000 | — |
| Reactant | 154632-86-7 | HCID 12344749 | — |
| Reactant | tert-Butyl [(cyclopropylmethyl)((2S)-2-hydroxy-2-phenylethyl)]carbamate | HCID 66939349 | — |
| Solvent | Chloroform | HCID 6212 | — |
| Product | Methyl N-[(benzyloxy)carbonyl]-O-{(1S)-2-[(tert-butoxycarbonyl) (cyclopropylmethyl)amino]-1-phenylethyl}-D-serinate | HCID 66939283 | 27.4% |
Reaction Steps
Boron trifluoride diethyl etherate (0.10 mL, 0.84 mmol) was added to a solution of tert-butyl cyclopropylmethyl[(2S)-2-hydroxy-2-phenylethyl]carbamate (2.45 g, 8.39 mmol) and 1-benzyl 2-methyl (2R)-aziridine-1,2-dicarboxylate (1.97 g, 8.39 mmol) in chloroform (20 mL). After 3 h, the reaction was concentrated. Purification by silica gel chromatography (100% hexanes→30% ethyl acetate/hexanes) gave the title compound (1.21 g).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07745427B2 |
| Source dataset | uspto-grants-2010_06 |
| ORD ID | ord-5b841593848844df94435d334de285f5 |
| Source note | uspto-grants-2010_06 |