HuagongsheHuagongshe Chemistry Print Report · For research reference only
Hydrogen Peroxide → 1-({(4r,7s,13s,16r)-7-(2-Amino-2-oxoethyl)-13-[(2s)-butan-2-yl]-16-(4-ethoxybenzyl)-10-[(1r)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl}carbonyl)-l-prolyl-l-ornithylglycinamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Hydrogen Peroxide | HCID 784 | — |
| Reactant | Atosiban | HCID 5311010 | — |
| Reactant | Azane;hydrate | HCID 12896473 | — |
| Solvent | Acetonitrile | HCID 6342 | — |
| Product | 1-({(4r,7s,13s,16r)-7-(2-Amino-2-oxoethyl)-13-[(2s)-butan-2-yl]-16-(4-ethoxybenzyl)-10-[(1r)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl}carbonyl)-l-prolyl-l-ornithylglycinamide | HCID 68613 | — |
Reaction Steps
2.85 g of atosiban acetate is prepared by dissolving the linear atosiban obtained from Example 2 in 250 ml of 5% acetonitrile aqueous solution, adjusting the pH value to 8 to 9 with 30% ammonia water, adding 0.60 g of H2O2, reacting for 10 min at 25° C., monitoring with HPLC (HPLC: 75.6%), filtering after reaction, purifying filtrate by preparative RP-HPLC (column C18 or C8), transferring salt, and freeze-drying, MS: 994.5, HPLC: 99.4%.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09434767B2 |
| Source dataset | uspto-grants-2016_09 |
| ORD ID | ord-1bcb029a3e0d49aa978b77f684bff4c5 |
| Source note | uspto-grants-2016_09 |