|
【结 构 式】 
|
【药物名称】(?-PPG 【化学名称】(±)-2-Amino-2-(4-phosphonophenyl)acetic acid 【CA登记号】120667-15-4, 120667-18-7 (hydrochloride) 【 分 子 式 】C8H10NO5P 【 分 子 量 】231.1464 |
【开发单位】Merck & Co. (Originator), Novartis (Originator) 【药理作用】Antiepileptic Drugs, Cerebrovascular Diseases, Treatment of, NEUROLOGIC DRUGS, Stroke, Treatment of, mglu8 Agonists |
合成路线1
Condensation of alpha-hydroxyhippuric acid (II) with bromobenzene (I) in methanesulfonic acid afforded the phenylglycine derivative (III). Further incorporation of the phosphonic acid was effected by palladium-catalyzed displacement of the bromide by diethyl phosphite to give (IV). Finally, acid hydrolysis of the benzamide and phosphite ester groups furnished the title compound.
| 【1】 Bigge, C.F.; et al.; Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists. J Med Chem 1989, 32, 7, 1580-90. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 13365 | Monobromobenzene; 1-Bromobenzene；Phenylbromide;bromobenzene | 108-86-1 | C6H5Br | 详情 | 详情 |
| (II) | 20606 | 2-(benzoylamino)-2-hydroxyacetic acid | 16555-77-4 | C9H9NO4 | 详情 | 详情 |
| (III) | 35750 | 2-(benzoylamino)-2-(4-bromophenyl)acetic acid | C15H12BrNO3 | 详情 | 详情 | |
| (IV) | 35751 | 2-(benzoylamino)-2-[4-(diethoxyphosphoryl)phenyl]acetic acid | C19H22NO6P | 详情 | 详情 |
Extended Information