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【结 构 式】 
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【药物名称】Efaproxiral sodium, RSR-13 【化学名称】2-[4-(3,5-Dimethylphenylcarbamoylmethyl)phenoxy]-2-methylpropionic acid sodium salt 【CA登记号】170787-99-2, 131179-95-8 (free acid) 【 分 子 式 】C20H22NNaO4 【 分 子 量 】363.39244 |
【开发单位】Virginia Commonwealth University (Originator), Allos (Codevelopment) 【药理作用】Acute Myocardial Infarction, Treatment of, Angina pectoris, Treatment of, Antineoplastic Enhancing Agents, CARDIOVASCULAR DRUGS, Cerebrovascular Diseases, Treatment of, Coronary Bypass Surgery, Modulators of the Therapeutic Activity of Antineoplastic Agents, NEUROLOGIC DRUGS, ONCOLYTIC DRUGS, Radiation Therapy, Radiosensitizers, Stroke, Treatment of, Treatment of Disorders of the Coronary Arteries and Atherosclerosis |
合成路线1
Reaction of 4-hydroxyphenylacetic acid (I) with refluxing SOCl2, followed by treatment of the resulting polymeric phenol ester with 3,5-dimethylaniline (II) in refluxing xylene provided amide (III). Condensation of this compound with acetone and chloroform in the presence of powdered NaOH yielded the corresponding isobutyric acid derivative.
| 【1】 McIntyre, J.; Castaner, J.; Efaproxiral Sodium. Drugs Fut 2003, 28, 12, 1159. |
| 【2】 Abraham, D.J.; Mehanna, A.; Randad, R.; Mahran, M.; Allosteric hemoglobin modifiers. US 5049695; WO 9112235 . |
| 【3】 Randad, R.S.; et al.; Allosteric modifiers of hemoglobin. 1. Design, synthesis, testing, and structure-allosteric activity relationship of novel hemoglobin oxygen affinity decreasing agents. J Med Chem 1991, 34, 2, 752. |