Actarit CAS 18699-02-0
Introduction：Basic information about Actarit CAS 18699-02-0, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Actarit Basic information
| Product Name: | Actarit |
| Synonyms: | 4-(acetylamino)-benzeneacetic acid;[4-(ACETYLAMINO)PHENYL]ACETIC ACID;(p-acetamidophenyl)-aceticaci;(p-acetamidophenyl)aceticacid;4-(acetylamino)-benzeneaceticaci;4-n-acetylaminophenylaceticacid;ms932;RARECHEM AL BO 1520 |
| CAS: | 18699-02-0 |
| MF: | C10H11NO3 |
| MW: | 193.2 |
| EINECS: | 242-511-3 |
| Product Categories: | Aromatic Phenylacetic Acids and Derivatives;Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol File: | 18699-02-0.mol |
Actarit Chemical Properties
| Melting point | 173-175°C |
| Boiling point | 449.1±28.0 °C(Predicted) |
| density | 1.288±0.06 g/cm3(Predicted) |
| storage temp. | Sealed in dry,Room Temperature |
| solubility | DMSO, Ethanol, Methanol |
| form | Solid |
| pka | 4.34±0.10(Predicted) |
| color | White to Off-White |
| Merck | 14,133 |
| CAS DataBase Reference | 18699-02-0(CAS DataBase Reference) |
Safety Information
| Safety Statements | 24/25 |
| RTECS | CY1542000 |
| HS Code | 29163990 |
| Toxicity | LD50 in male, female mice, male, female rats (mg/kg): 1.06, 1.30, 1.95, 2.03 i.p.; 5.68, 5.48, 5.48, 6.12 s.c.; 15.3, 14.7, 14.8, 15.4 orally (Toshida) |
| Description | Actarit is an orally administered disease-modifying antirheumatic drug launched inJapan. Although its structure resembles that of non-steroidal anti-inflammatorydrugs, it has no effect on experimental acute inflammation and has no analgesic orantipyretic effects. Its preventative and therapeutic effects on adjuvant arthritis aremediated via modulation of production and serum level of interleukin-2 whichenhances production of suppressor T-cells to the immune system, thereby,preventing development of articular lesions. |
| Chemical Properties | Crystalline Solid |
| Originator | Nippon Shlnyaku;Mltaublshl Kasel (Japan) |
| Uses | Antiarthritic |
| Uses | Chronic rheumatoid arthritis |
| Definition | ChEBI: Actarit is an anilide and a member of acetamides. |
| Brand name | Orcl; Mover |
| Synthesis | 1197-55-3 108-24-7 18699-02-0 General procedure: 1.02 mmol of p-aminophenylacetic acid (Wako Pure Pharmaceutical Industries, Ltd.) was dissolved in 50 mL of a solvent mixture of dichloromethane-methanol-water (1:3:1, v/v). Under ice bath cooling conditions, 2.12 mmol of acetic anhydride was slowly added. The reaction mixture was gradually brought to room temperature with stirring and continued to stir overnight. Upon completion of the reaction, the solvent was removed by distillation under reduced pressure to give 196.4 mg of 2-(4-acetylaminophenyl)acetic acid in 99% yield. The structure of the product was confirmed by 1H-NMR (500 MHz, CD3OD): δ 2.11 (3H, s, Ac), 3.55 (2H, s, Ph-CH2-), 7.21-7.49 (4H, m, aromatic H). |
| Purification Methods | Crystallise the acid from MeOH/Me2CO, aqueous EtOH or H2O. The amide has m 231o (from 50% aqueous EtOH). [Gabriel Chem Ber 15 841 1882, Cerecedo et al. J Biol Chem 42 238 1924, Tramontano et al. J Am Chem Soc 110 2282 1988, Beilstein 14 II 281.] |
| References | [1] Patent: EP3363463, 2018, A2. Location in patent: Paragraph 0148 [2] Asian Journal of Chemistry, 2012, vol. 24, # 4, p. 1538 - 1540 [3] Journal of the American Chemical Society, 1988, vol. 110, # 7, p. 2282 - 2286 [4] Journal of the American Chemical Society, 2009, vol. 131, p. 456 - 457 [5] Patent: WO2015/145371, 2015, A1. Location in patent: Page/Page column 40 |
Actarit Preparation Products And Raw materials
| Raw materials | N,N-Dimethylacetamide-->4-Aminophenylacetic acid-->Acetic anhydride-->Acetic acid |
| Preparation Products | (4-Amino-3-chloro-phenyl)-acetic acid methyl ester-->2-(4-ACETAMIDO-3-NITROPHENYL)ACETIC ACID |
