Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | HCID 10580420 | HCID 10580420 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | HCID 22940458 | HCID 22940458 | — |
Reaction Steps
Under a nitrogen atmosphere, 200 mg (0.293 mmol) of 1-[4-(2-tert-butyl-2H-tetrazol-5-yl)-phenyl]-4(S)-hydroxy-5(S)-N-(tert-butyloxycarbonyl)amino-2-N-[N-methoxycarbonyl-(L)-tert-leucyl]amino-6-phenyl-2-azahexane are dissolved in 2.3 ml of THF; 1.6 ml of aqueous 2N HCl are added and the mixture is stirred at 50° C. for 8 hours. The reaction solution is concentrated by evaporation; the residue is taken up several times in ethanol and concentrated by evaporation again (→title compound): TLC: Rt =0.08 (CH2Cl2 /MeOH 30:1); HPLC20-100(12') : tRet =9.9; 1H-NMR (CD3OD) d 8.03 and 7.50 (2d, J=8, each 2H), 7.32 (m, 5H), 4.18 and 3.91 (2d, J=4, 2H), 3.80 (m, 1H), 3.68 (s, 1H), 3.58 (s, 3H), 3.57 (m, 1H), 3.3-2.9 (m, 4H), 1.81 and 0.75 (2s, each 9H).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US05849911 |
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| Source dataset | uspto-grants-1998_12 |
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| ORD ID | ord-ef8c15d64f874056a98227c82bc158f9 |
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| Source note | uspto-grants-1998_12 |
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