Naltrexone Base → Benzyl Alcohol

HRID 1508010

Reaktionsgleichung

Reaktionsgleichung von HRID 1508010
[CH2:1]1[CH:3]([CH2:4][N:5]2[C@@H:15]3[CH2:16][C:17]4[CH:22]=[CH:21][C:20]([OH:23])=[C:19]5[O:24][CH:9]6[C:10]([CH2:12][CH2:13][C@:14]3([OH:25])[C@:8]6([C:18]=45)[CH2:7][CH2:6]2)=[O:11])[CH2:2]1>C(O)C1C=CC=CC=1>[CH2:2]1[CH:3]([CH2:4][N:5]2[CH:15]3[CH2:16][C:17]4[CH:22]=[CH:21][C:20]([OH:23])=[C:19]5[O:24][CH:9]6[C:10]([CH2:12][CH2:13][C:14]3([OH:25])[C:8]6([C:18]=45)[CH2:7][CH2:6]2)=[O:11])[CH2:1]1.[CH2:19]([OH:24])[C:18]1[CH:8]=[CH:14][CH:15]=[CH:16][CH:17]=1

Komponenten

4

Edukt 1

HCID 21159611Naltrexone Base

Produkt 2

HCID 244Benzyl AlcoholAusbeute 70 %HCID 44283-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-oneAusbeute 30 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 244Benzyl AlcoholLösungsmittel

Versuchsvorschrift

A 1 kg batch of naltrexone microspheres were prepared as follows. Polymer solution was formed by dissolving 75:25 DL PLGA (poly(lactide)-co-glycolide) in ethyl acetate (EtAc) to form a solution of 16.7% polymer and 83.3% EtAc. A naltrexone solution was formed by dissolving naltrexone base in benzyl alcohol (BA) to form a solution of 30% naltrexone base anhydrous and 70% BA. The polymer solution and the naltrexone solution were mixed together to form a drug/polymer solution that was the “organic” or “oil” phase of the emulsion.

Quellen und Nachweise

ORD-Eintrag
ord-17e634018c2144318a8ecbaf518c7585
Quelldatensatz
uspto-grants-2015_12
Patentnummer
US09221830B2

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