TMC207 CAS 843663-66-1 Purity >99.5% (HPLC)
TMC207 Related Intermediates:
TMC207 CAS 843663-66-1
3-Benzyl-6-Bromo-2-Chloroquinoline CAS 654655-68-2
3-Benzyl-6-Bromo-2-Methoxyquinoline CAS 654655-69-3
| Chemical Name | TMC207 |
| Synonyms | TMC-207, R207910; Sirturo; (αS,βR)-6-Bromo-α-[2-(dimethylamino)ethyl]-2-methoxy-α-1-naphthalenyl-β-phenyl-3-Quinolineethanol; 1-(6-Bromo-2-methoxyquinolin-3-yl)-4-dimethylamino-1-phenyl-2-(1-naphthyl) 2-butanol |
| CAS Number | 843663-66-1 |
| CAT Number | RF2336 |
| Stock Status | In Stock, Production Scale Up to Tons |
| Molecular Formula | C32H31BrN2O2 |
| Molecular Weight | 555.516 |
| Melting Point | 104℃ |
| Density | 1.322±0.06 g/cm3 |
| Sensitive | Hygroscopic. Light Sensitive, Air Sensitive |
| Brand | Ruifu Chemical |
| Item | Specifications |
| Appearance | White or Off-White Powder |
| Purity / Analysis Method | >99.5% (HPLC) |
| Loss on Drying | <0.50% |
| Residue on Ignition | <0.20% |
| Any Individual Impurity | <0.10% |
| Isomer | <0.10% |
| Total Impurities | <0.50% |
| Heavy Metals (as Pb) | <20ppm |
| Arsenic (As) | <2.0ppm |
| Infrared Spectrum | Conforms to Structure |
| Proton NMR Spectrum | Conforms to Structure |
| Test Standard | Enterprise Standard |
| Usage | API |
Package: Bottle, Aluminum foil bag, 25kg/Cardboard Drum, or according to customer's requirement
Storage Condition: Store in sealed containers at cool and dry place; Protect from light and moisture
How to Purchase? Please contact: sales@ruifuchem.com or alvin@ruifuchem.com
15 Years Experience? We have more than 15 years of experience in the manufacture and export of a wide range of high quality pharmaceutical intermediates or fine chemicals.
Main Markets? Mainly exported to North America, India, Russia, Korea, Japanese, and Europe, etc.
Quality Assurance? Reliable quality assurance, strict management. Professional equipment for analysis include NMR, LC-MS, GC, HPLC, ICP-MS, UV, IR, OR, K.F, ROI, LOD, MP, Clarity, Solubility, Microbial limit test, etc.
Samples? Most products provide free samples for quality evaluation, shipping cost should be paid by customers.
Factory Audit? Factory audit welcome. Please make an appointment in advance.
MOQ? No MOQ. Small order is acceptable.
Delivery Time? If within stock, three days delivery guaranteed.
Transportation? By Express (FedEx, DHL), by Air, by sea.
Custom Synthesis? Can provide custom synthesis services.
Payment Terms? Proforma invoice will be sent first after confirmation of order, enclosed our bank information. Payment by T/T (Telex Transfer), PayPal, Western Union, etc.
(CAS: 843663-66-1), (known as TMC207 and R207910), traded under the trade name Sirturo, is a novel diarylquinoline antimycobacterial drug that affects tuberculosis by inhibiting the activity of the M. tuberculosis ATP synthase proton pump. The ATP synthesis of mycobacteria exerts antibacterial and bactericidal effects. Clinically used to treat adult multidrug-resistant tuberculosis (MDR-PTB). TMC207 has the same bactericidal activity against M. tuberculosis sensitive strains and resistant strains, and also has good sterilization effect on dormant bacteria. In December 2012, the US FDA approved TMC207 as part of combination therapy for the treatment of multi-drug resistant tuberculosis (MDRTB). TMC207 is the first drug approved for MDR-TB and is the first approval from a new class of antituberculosis agents in the past 40 years. Due to the high unmetmedical need for treating MDR-TB, the FDA granted TMC207 accelerated approval based on Phase II results, providing patients access to the drug while additional clinical studies are carried out. TMC207 is a diarylquinoline that was discovered from a high-throughput, whole-cell screening strategy with Mycobacterium smegmatis used as a surrogate for M. tuberculosis. TMC207 is a single enantiomer of an initial screening hit. TMC207 has potent and selective activity against mycobacteria, and is active against both drug-sensitive and drug-resistant M. tuberculosis. The mechanism of action of TMC207 is unique amongst anti-TB drugs and involves inhibition of mycobacterial ATP synthase; it is not active against human ATP synthase. TMC207 has in vivo activity in numerous preclinical models of TB infection, alone and in combination with other anti-TB agents, and has bactericidal activity in established TB infection models. TMC207 is synthesized in five steps from 3-Phenylpropionic Acid and para-Bromoaniline. Following amide formation, treatment with POCl3 and DMF under Vilsmeier-Hack conditions gave a 2-Chloroquinoline product. Treatment with sodium methoxide, followed by condensation with 3-(Dimethylamino)-1-(naphthalen-1-yl)propan-1-one, and separation of isomers gave TMC207.
