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【结 构 式】 
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【药物名称】 【化学名称】5-(1-Piperidinyl)-5H-1-benzopyran[4,3-d]pyrimidin-2-amine 【CA登记号】 【 分 子 式 】C16H18N4O 【 分 子 量 】282.34806 |
【开发单位】Università degli Studi di Genova (Originator), Università degli Studi di Parma (Originator) 【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Antiplatelet Therapy, Antipyretics, Coagulation Disorders Therapy, HEMATOLOGIC DRUGS, Non-Opioid Analgesics, Non-Steroidal Antiinflammatory Drugs |
合成路线1
3-Formylchromen-4-one (II) was prepared by Vilsmeier formylation of 2'-hydroxyacetophenone (I) with POCl3 and DMF. Cyclization of (II) with guanidine carbonate (III) in refluxing EtOH gave rise to the benzopyranopyrimidine (IV). This was finally condensed with piperidine (V) in the presence of TiCl4 to furnish the title compound.
| 【1】 Barocelli, E.; Bertoni, S.; Bruno, O.; Ranise, A.; Schenone, S.; Chiavarini, M.; Ballabeni, V.; Synthesis and pharmacological screening of novel non-acidic gastroprotective antipyretic anti-inflammatory agents with anti-platelet properties. 5-Alkyl/cycloalkylamino substituted 2-amino-5H-[1]benzopyrano[4,3-d]pyrimidines. Arzneim-Forsch Drug Res 2000, 50, 2, 140. |
| 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) | 29654 | 2-hydroxyacetophenone; 1-(2-hydroxyphenyl)-1-ethanone | 118-93-4 | C8H8O2 | 详情 | 详情 |
| (II) | 47086 | 4-oxo-4H-chromene-3-carbaldehyde | 17422-74-1 | C10H6O3 | 详情 | 详情 |
| (III) | 14790 | Guanidine | 113-00-8 | CH5N3 | 详情 | 详情 |
| (IV) | 47087 | 2-amino-5H-chromeno[4,3-d]pyrimidin-5-ol | C11H9N3O2 | 详情 | 详情 | |
| (V) | 10158 | Piperidine | 110-89-4 | C5H11N | 详情 | 详情 |