2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
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- CAS-Nr.
- 594839-88-0
- Englisch Name:
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- Synonyma:
- TafaMidis;Fx-1006A;Fx 1006;Fx1006A;Fx 1006A;Tafamidis API;Chlorfenazolac;Tafamidis(Fx 1006);afamidis (Fx1006A);Tafamidis free acid
- CBNumber:
- CB52484674
- Summenformel:
- C14H7Cl2NO3
- Molgewicht:
- 308.12
- MOL-Datei:
- 594839-88-0.mol
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2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Eigenschaften
- Siedepunkt:
- 486.7±40.0 °C(Predicted)
- Dichte
- 1.530
- storage temp.
- -20°
- L?slichkeit
- Soluble in DMSO (up to 20 mg/ml).
- Aggregatzustand
- solid
- pka
- 3.49±0.30(Predicted)
- Farbe
- Off-white
- Stabilit?t:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P302+P352 |
BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P321 |
Besondere Behandlung |
| P332+P313 |
Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P362 |
Kontaminierte Kleidung ausziehen und vor erneutem Tragen waschen. |
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2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (K
d1 = 3 nM; K
d2 = 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC
50s = 2.7-3.2 μM) under fibril-promoting, denaturing, and physiological conditions
in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits
ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 μM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.
Verwenden
Tafamidis can be used as a benzoxole derivative that is a transthyretin (TTR) amyloid fibril inhibitors. It is a new drug candidate in the treatment of TTR amyloidosis (caused my misfolding of proteins).
Definition
ChEBI: A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazole-6-carboxylic acid in which the hydrogen at position 2 is replaced by a 3,5-dichlorophenyl group. Used (as its meglumine salt) for the amelioration of transthyretin-related hereditary amyloid
sis.
Synthese
The synthesis of 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid is as follows:
methyl 2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylate (17.9 mmol) was dissolved in a mixture of THF:MeOH:H2O (3:1:1, 50 mL) and treated with LiOH (71.6 mmol) at room temperature for 6h. The mixture was acidified to pH 2 with 1 N HCl and extracted with EA. The combined organic layers were dried over MgSO4, filtered and concentrated to give the product as a white solid 5.0 g, yield 91%.
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 147)Lieferanten
594839-88-0()Verwandte Suche:
- Fx 1006
- 6-Benzoxazolecarboxylic acid, 2-(3,5-dichlorophenyl)-
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- Tafamidis (Fx1006A)
- Tafamidis free acid
- PF-06291826(Tafamidis)
- Tafamidis(Fx 1006)
- Fx 1006A
- Fx1006A
- FX-1006A;FX1006A;FX 1006A
- Tafamidis free acid, 2-(3,5-dichlorophenyl)-6-benzoxazole carboxylic acid
- TafaMidis
- Fx-1006A
- 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid
- afamidis (Fx1006A)
- 2-(3,5-Dichlorophenyl)benzoxazole-6-carboxylic Acid
- Tafamidis API
- 2-(3,5-Dichlorophenyl)-1,3-Benzoxazole-6-carboxylic acid
- Chlorfenazolac
- 594839-88-0
- Aromatics
- Heterocycles
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- API
