Sodium Hydroxide → Bortezomib Catechol

HRID 574053Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 574053
[B:1]([OH:28])([OH:27])[C@@H:2]([NH:7][C:8]([C@@H:10]([NH:18][C:19]([C:21]1[CH:22]=[N:23][CH:24]=[CH:25][N:26]=1)=[O:20])[CH2:11][C:12]1[CH:13]=[CH:14][CH:15]=[CH:16][CH:17]=1)=[O:9])[CH2:3][CH:4]([CH3:6])[CH3:5].Cl.NCC[C:33]1[CH:40]=[CH:39][C:37]([OH:38])=[C:35]([OH:36])[CH:34]=1.P(O)(O)([O-])=O.[Na+].[OH-].[Na+]>>[B:1]([OH:28])([OH:27])[C@@H:2]([NH:7][C:8]([C@@H:10]([NH:18][C:19]([C:21]1[CH:22]=[N:23][CH:24]=[CH:25][N:26]=1)=[O:20])[CH2:11][C:12]1[CH:17]=[CH:16][CH:15]=[CH:14][CH:13]=1)=[O:9])[CH2:3][CH:4]([CH3:6])[CH3:5].[C:35]1([C:37](=[CH:39][CH:40]=[CH:33][CH:34]=1)[OH:38])[OH:36]

Komponenten

5

Edukt 4

HCID 14798Sodium HydroxideHCID 65340Dopamine HydrochlorideHCID 387447BortezomibHCID 23672064Monosodium phosphate

Produkt 1

HCID 131732842Bortezomib Catechol

Versuchsvorschrift

Bortezomib and dopamine hydrogen chloride were dissolved separately in d6-DMSO 0.2 M concentration. The two solutions were mixed to give a stock solution of DA-BTZ conjugate at 0.1 M in DMSO. A solution of 0.1 M monosodium phosphate in D2O was used to dilute the DA-BTZ stock to 1 mM, and pH of such solutions were adjusted with 4N NaOH in D2O to 5.5, 6.5, 7.4 and 8.5. These solutions were analyzed on AVANCE III 500 MHz (FIG. 6) and peak integrals in the range of 7.2 to 5.5 ppm were used for quantifying the degree of dissociation of DA-BTZ presented in FIG. 3B.

Aufarbeitung

  1. concentrationconcentration
  2. additionThe two solutions were mixed
  3. customto give a stock solution of DA-BTZ conjugate at 0.1 M in DMSO
  4. additionto dilute the DA-BTZ stock to 1 mM, and pH of such solutions

Quellen und Nachweise

ORD-Eintrag
ord-3dbc587fb160424f9a3c540788862735
Quelldatensatz
uspto-grants-2015_05
Patentnummer
US09034829B1

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