Réaction #8665

ord-06779464f394458c84c4a69fb56ae04b

Équation de réaction

C/C1=C/C[C@@H](/C(C)=C/c2csc(C)n2)OC(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC1

epothilone D

mannitol

epothilone D

CC(O)COC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@H]5[C@H](O)[C@@H](O)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O[C@H]8[C@H](O)[C@@H](O)[C@@H](O[C@H]1[C@H](O)[C@H]2O)O[C@@H]8COCC(C)O)O[C@@H]7COCC(C)O)O[C@@H]6COCC(C)O)O[C@@H]5COCC(C)O)O[C@@H]4COCC(C)O)O[C@@H]3COCC(C)O

hydroxypropyl-β-cyclodextrin

epothilone D

mannitol

epothilone D

→

C/C1=C/C[C@@H](/C(C)=C/c2csc(C)n2)OC(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC1.CC(O)COC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@H]5[C@H](O)[C@@H](O)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O[C@H]8[C@H](O)[C@@H](O)[C@@H](O[C@H]1[C@H](O)[C@H]2O)O[C@@H]8COCC(C)O)O[C@@H]7COCC(C)O)O[C@@H]6COCC(C)O)O[C@@H]5COCC(C)O)O[C@@H]4COCC(C)O)O[C@@H]3COCC(C)O

Epothilone D Hydroxypropyl-β-Cyclodextrin

Réactifs

epothilone D

mannitol

epothilone D

hydroxypropyl-β-cyclodextrin

Réactifs

Aucun

Solvants

tert-butanol water

Conditions de réaction

Conditions détaillées

See reaction.notes.procedure_details.

Traitement

1
Autrewas prepared

Mode opératoire

A combination of ten milligrams (“mg”) of epothilone D and 0.4 grams (“g”) of hydroxypropyl-β-cyclodextrin (“HPβCD”) were dissolved in 60% tert-butanol-water to make 1 milliliter (“mL”) of solution. A second solution having ten mg of epothilone D and ten mg of mannitol dissolved in 60% tert-butanol-water was prepared. A third solution of ten mg of epothilone D and ten mg of mannitol in 60% tert-butanol-water was also prepared. Formulation solutions containing ten mg/mL epothilone D were poured into 8 mL glass vials for lyophilization.

Source

DOI: 10.6084/m9.figshare.5104873.v1Brevet: US07091193B2uspto-grants-2006_08