2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- CAS No.
- 594839-88-0
- Chemical Name:
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- Synonyms
- TafaMidis;Fx-1006A;Fx 1006;Fx1006A;Fx 1006A;Tafamidis API;Tafamidis(Fx 1006);afamidis (Fx1006A);Tafamidis free acid;Tafamidis (Fx1006A)
- CBNumber:
- CB52484674
- Molecular Formula:
- C14H7Cl2NO3
- Molecular Weight:
- 308.12
- MOL File:
- 594839-88-0.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/3/22 14:56:24
| Boiling point | 486.7±40.0 °C(Predicted) |
|---|---|
| Density | 1.530 |
| storage temp. | -20° |
| solubility | Soluble in DMSO (up to 20 mg/ml). |
| form | solid |
| pka | 3.49±0.30(Predicted) |
| color | Off-white |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H335-H319-H315 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P | |||||||||
| NFPA 704 |
|
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Chemical Properties,Uses,Production
Description
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (Kd1 = 3 nM; Kd2 = 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 (EC50s = 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.
Uses
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.
Synthesis
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 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| GLP Pharma Standards | +91 9866074638 | Hyderabad, India | 1644 | 58 | Inquiry |
| Synaptics Labs Private Limited | +91-8341963666 +91-8341963666 | Hyderabad, India | 84 | 58 | Inquiry |
| Biophore India Pharmaceuticals Pvt Ltd | +91-9100031592 +91-9030907714 | Telangana, India | 134 | 58 | Inquiry |
| Virupaksha Organics Pvt Ltd | +91-9440049755 +91-9848648601 | Telangana, India | 40 | 58 | Inquiry |
| Aruvi Labs | +91-8056181939 +91-8056181939 | Tamil Nadu, India | 149 | 58 | Inquiry |
| Venkatasai Life Sciences | +91-9908134868 +91-8008303069 | Hyderabad, India | 186 | 58 | Inquiry |
| Nuray Chemicals Pvt Ltd | +91-4066616700 +91-8220444745 | Tamil Nadu, India | 49 | 58 | Inquiry |
| MSN LABORATORIES PRIVATE LTD | +91 40 30438600 | New Delhi, India | 230 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
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