核苷中间体
核苷中间体在药物合成中扮演着重要角色，特别是在抗病毒和抗癌药物的开发中。这些化合物通常用于合成最终的活性物质。核苷是一类含糖结构的重要生物分子，在体内参与DNA和RNA的构成与代谢。
核苷中间体是指从基本原料出发，通过一系列化学反应合成得到的、接近或直接作为后续步骤前驱体的化合物。它们在药物研发过程中至关重要，因为这些中间体可以提供更便捷的方法来引入特定官能团或结构片段，从而简化整个合成路线，提高产率并减少副产品的生成。
核苷中间体的合成通常包括以下几个关键步骤：
- 糖基化反应：从简单的糖（如葡萄糖、半乳糖等）开始，通过糖基化反应引入特定类型的糖分子。
- 修饰与转化：对所得的糖结构进行进一步的化学修饰或转化。这可能涉及磷酸化、糖苷化或其他官能团的引入，以形成最终的核苷化合物。
- 脱保护与纯化：通过适当的脱保护策略和纯化技术获得所需的核苷中间体。
这些中间体在合成过程中具有高度选择性和反应性，在特定条件下能够精确地进行化学转化。因此，它们对于确保目标产品的高质量生产和高效开发至关重要。此外，不同类型的核苷中间体可以用于制备不同的药物分子，如抗病毒药物（例如阿昔洛韦）、抗癌药物以及其他多种生物活性物质。
| 中文名称 | 英文名称 | CAS号 | 化学式 |
|---|---|---|---|
| —— | O<sup>(</sup>2-2')-Anhydro-uridin | 3736-77-4 | C9H10N2O5 |
| —— | (4R,5R,6S)-5-hydroxy-4-(hydroxymethyl)-3,7-dioxa-1,9-diazatricyclo[6.4.0.02,6]dodeca-8,11-dien-10-one | 3736-77-4 | C9H10N2O5 |
| —— | 9-(beta-D-Ribofuranosyl)zeatin | 6025-53-2 | C15H21N5O5 |
| —— | [(4aR,7R,7aR)-6-[6-(butanoylamino)purin-9-yl]-2-hydroxy-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-yl] butanoate | 362-74-3 | C18H24N5O8P |
| —— | α-2-thioribouridine | 13255-58-8 | C9H12N2O5S |
| —— | 5-Fluoro-1-((2R,3R,4R,5R)-3,4,5-trihydroxytetrahydro-2H-pyran-2-yl)pyrimidine-2,4(1H,3H)-dione | 77180-80-4 | C9H11FN2O6 |
| —— | 6-thio-inosine | 574-25-4 | C10H12N4O4S |
| —— | 2'C-methylcytidine | 20724-73-6 | C10H15N3O5 |
| —— | 4-N-Acetylcytidine | 3768-18-1 | C11H15N3O6 |
| —— | uridine-3'-phosphate disodium salt | 35170-03-7 | C9H11N2O9P*2Na |
| —— | (2S,3S,4R,5S)-2-(2-aminopurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol | 4546-54-7 | C10H13N5O4 |
| —— | [(3R,4R,5R)-2-(6-aminopurin-9-yl)-4-hydroxy-5-(hydroxymethyl)oxolan-3-yl] dihydrogen phosphate | 130-49-4 | C10H14N5O7P |
| —— | Adenosine 5'-monophosphate xsodium salt | 1231926-40-1 | C10H14N5NaO7P |
| —— | 3387-36-8 | C9H13N2NaO9P | |
| —— | sodium;[(3aS,4R,6R,6aS)-4-(6-aminopurin-9-yl)-2-oxido-2-oxo-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3,2]dioxaphosphol-6-yl]methanol | 37063-35-7 | C10H11N5NaO6P |
| —— | β-DL-Isopropylideninosin | 2140-11-6 | C13H16N4O5 |
| —— | 1-(6-amino-purin-9-yl)-<i>O</i><sup>2'</sup>-phosphono-α-<i>L</i>-1-deoxy-lyxofuranose | 130-49-4 | C10H14N5O7P |
| —— | 4-amino-1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidin-2(1H)-one | 2140-61-6 | C10H15N3O5 |
| —— | L-guanosine | 26578-09-6 | C10H13N5O5 |
| —— | 2-amino-9-(<i>O</i><sup>2</sup>,<i>O</i><sup>3</sup>-isopropylidene-β-<i>D</i>-lyxofuranosyl)-1,9-dihydro-purin-6-one | 362-76-5 | C13H17N5O5 |
| —— | [(2R,3R,4S,5R)-3,4-dibenzoyloxy-5-cyanooxolan-2-yl]methyl benzoate | 23316-67-8 | C27H21NO7 |
| —— | <i>N</i><sup>α</sup>-(<i>N</i>-benzyloxycarbonyl-glycyl)-histidine | 38972-84-8 | C16H18N4O5 |
| —— | (4aS,6R,7R,7aR)-6-(6-amino-8-bromopurin-9-yl)-2-hydroxy-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol | 23583-48-4 | C10H11BrN5O6P |
| —— | N4-aminocytidine | 57294-74-3 | C9H14N4O5 |
| —— | US10874683, Example EIDD-01910-01 | 57294-74-3 | C9H14N4O5 |
| —— | 5'-Inosinic acid, sodium salt, hydrate (1:2:8) | 20813-76-7 | C10H27N4Na2O16P |
| —— | Disodium guanosine triphosphate | 56001-37-7 | C10H16N5O14P3 |
| —— | 2'3'-Isopropylidene-adenosine | 362-75-4 | C13H17N5O4 |
| —— | Guanosine-5'-triphosphate (disodium salt) | —— | C10H14N5Na2O14P3 |
| —— | 2-{[Hydroxy(phenyl)methylidene]amino}-9-pentofuranosyl-9H-purin-6-ol | 3676-72-0 | C17H17N5O6 |
| —— | 1-(6-amino-purin-9-yl)-<i>O</i><sup>2</sup>,<i>O</i><sup>3</sup>-isopropylidene-α-<i>D</i>-1-deoxy-lyxofuranose | 362-75-4 | C13H17N5O4 |
| —— | <i>O</i><sup>2'<sub>,<i>O</i></sub>3'</sup>-isopropylidene-adenosine | 362-75-4 | C13H17N5O4 |
| —— | 2-hydroxymethyl-3-hydroxytetrahydrofuran (2RS, 3SR) | 91121-19-6 | C5H10O3 |
| —— | uridine 3'-monophosphate | 35170-03-7 | C9H11N2O9P |
| —— | 2',3'-cAMP*Na | 37063-35-7 | C10H11N5O6P*Na |
| —— | 6-((E)-4-hydroxy-3-methylbut-2-enylamino)-9-β-D-ribofuranosylpurine | 6025-53-2 | C15H21N5O5 |
| —— | 9-ribosyl-trans-zeatin | 6025-53-2 | C15H21N5O5 |
| —— | 8-bromoadenosine 3′,5′-cyclic monophosphate | 23583-48-4 | C10H11BrN5O6P |
| —— | adenosine 3',5'-(cyclic)phosphate monosodium salt | 37839-81-9 | C10H11N5O6P*Na |
| —— | 2',3'-isopropylideneadenosine | 362-75-4 | C13H17N5O4 |
| —— | Vidarabine Sodium Phosphate | 132-00-3 | C10H12N5O7P*2Na |
| —— | 3'-O-(tert-butyldimethylsilyl)-2'-deoxyuridine | 76223-05-7 | C15H26N2O5Si |
| —— | 8-aminoguanosine | 3868-32-4 | C10H14N6O5 |
| —— | 2,3,5-tri-O-benzoyl-β-D-ribofuranosyl-1-carbonitrile | 23316-67-8 | C27H21NO7 |
| —— | 1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-4-sulfanylidenepyrimidin-2-one | 13957-31-8 | C9H12N2O5S |
| —— | 2,6-Diaminopurine riboside | 24649-67-0 | C10H14N6O4 |
| —— | 4-Amino-5-methyl-1-pentofuranosyl-2(1h)-pyrimidinone | 2140-61-6 | C10H15N3O5 |
| —— | 5'-Trityluridine | 6554-10-5 | C28H26N2O6 |
| —— | <i>O</i><sup>2'<sub>,<i>O</i></sub>3'</sup>-isopropylidene-guanosine | 362-76-5 | C13H17N5O5 |
| —— | 6-azauridine | 54-25-1 | C8H11N3O6 |
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