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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:

  1. 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。
  2. 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。
  3. 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 结构式图片
2-氨基-4-羟基吡咯并[2,3-d]嘧啶 2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one 7355-55-7 C6H6N4O
2-氨基-4-羟基吡咯并[2,3-d]嘧啶
2-氨基-4-氯吡咯并[2,3-d]嘧啶 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-amine 84955-31-7 C6H5ClN4
2-氨基-4-氯吡咯并[2,3-d]嘧啶
2-氨基-3,5-二氢吡咯并[3,2-D]嘧啶-4-酮 9-deazaguanine 65996-58-9 C6H6N4O
2-氨基-3,5-二氢吡咯并[3,2-D]嘧啶-4-酮
2-氟腺苷 2-fluoroadenosine 146-78-1 C10H12FN5O4
2-氟腺苷
2-C-甲基鸟苷 2'-C-methylguanosine 374750-30-8 C11H15N5O5
2-C-甲基鸟苷
2,6-二氯嘌呤核苷 2,6-dichloropurine riboside 13276-52-3 C10H10Cl2N4O4
2,6-二氯嘌呤核苷
2,6-二巯基嘌呤 2,6-Dimercapto-purin 5437-25-2 C5H4N4S2
2,6-二巯基嘌呤
2,2'-脱水尿苷 2,2'-Anhydrouridine 3736-77-4 C9H10N2O5
2,2'-脱水尿苷
2'-甲氧基鸟苷 2'-O-methylguanosine 2140-71-8 C11H15N5O5
2'-甲氧基鸟苷
2'-甲氧基胞苷 2'-O-methylcytidine 2140-72-9 C10H15N3O5
2'-甲氧基胞苷
2'-甲氧基尿苷 2'-O-methyluridine 2140-76-3 C10H14N2O6
2'-甲氧基尿苷
2'-氨基-2'-脱氧胞苷 2'-amino-2'-deoxycytidine 26889-42-9 C9H14N4O4
2'-氨基-2'-脱氧胞苷
2'-O-甲基腺苷 2'-O-methyl adenosine 2140-79-6 C11H15N5O4
2'-O-甲基腺苷
2'-C-甲基胞嘧啶核苷 2'-C-methylcytidine 20724-73-6 C10H15N3O5
2'-C-甲基胞嘧啶核苷
2',3'-异丙叉腺苷 2',3'-isopropylidene adenosine 362-75-4 C13H17N5O4
2',3'-异丙叉腺苷
2',3'-O-异丙叉肌苷 2',3'-O-isopropylideneinosine 2140-11-6 C13H16N4O5
2',3'-O-异丙叉肌苷
2',3'-O-异丙亚基鸟苷 2',3'-isopropylideneguanosine 362-76-5 C13H17N5O5
2',3'-O-异丙亚基鸟苷
2',3',5'-三乙酰鸟苷 2',3',5'-tri-O-acetyl-guanosine 6979-94-8 C16H19N5O8
2',3',5'-三乙酰鸟苷
2',3',5'-三乙酰腺苷 triacetyladenosine 7387-57-7 C16H19N5O7
2',3',5'-三乙酰腺苷
2',3',5'-三乙酰肌苷 N-benzyloxycarbonylglycylhistidine 38972-84-8 C16H18N4O5
2',3',5'-三乙酰肌苷
2',3',5'-三乙酰尿苷 Tri-O-acetyluridine 4105-38-8 C15H18N2O9
2',3',5'-三乙酰尿苷
2',3',5'-三-O-乙酰-2-氨基-6-氯嘌呤核苷 [3,4-Diacetyloxy-5-(2-amino-6-chloropurin-9-yl)oxolan-2-yl]methyl acetate 16321-99-6 C16H18ClN5O7
2',3',5'-三-O-乙酰-2-氨基-6-氯嘌呤核苷
1-氰基-2,3,5-三苯甲酰氧基-beta-D-呋喃核糖 (3,4-Dibenzoyloxy-5-cyanooxolan-2-yl)methyl benzoate 23316-67-8 C27H21NO7
1-氰基-2,3,5-三苯甲酰氧基-beta-D-呋喃核糖
1-叠氮基-2,3,5-三苯甲酰氧基-beta-D-呋喃核糖 2,3,5-tri-O-benzoyl-β-D-ribofuranosyl azide 7408-41-5 C26H21N3O7
1-叠氮基-2,3,5-三苯甲酰氧基-beta-D-呋喃核糖
1-beta-D-阿拉伯呋喃糖基-5-溴尿嘧啶 bromouridine 957-75-5 C9H11BrN2O6
1-beta-D-阿拉伯呋喃糖基-5-溴尿嘧啶
1-((2R,3r,4r,5r)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-4-羟基-3-甲氧基四氢呋喃-2-基)嘧啶-2,4(1h,3h)-二酮 5'-O-(4,4'-dimethoxytrityl)-2'-O-methyluridine 103285-22-9 C31H32N2O8
1-((2R,3r,4r,5r)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-4-羟基-3-甲氧基四氢呋喃-2-基)嘧啶-2,4(1h,3h)-二酮
1,2-二脱氧-D-核糖 (2R,3S)-2-(hydroxymethyl)tetrahydrofuran-3-ol 91547-59-0 C5H10O3
1,2-二脱氧-D-核糖
—— D-Arabinosyl-5-fluorcytosin 2341-22-2 C9H12FN3O5
D-Arabinosyl-5-fluorcytosin
—— Sodium N-(9-{6-[(butanoyloxy)methyl]-2-hydroxy-2-oxotetrahydro-2H-2lambda~5~-furo[3,4-d][1,3,2]dioxaphosphol-4-yl}-9H-purin-6-yl)butanimidate 16980-89-5 C18H23N5NaO8P
Sodium N-(9-{6-[(butanoyloxy)methyl]-2-hydroxy-2-oxotetrahydro-2H-2lambda~5~-furo[3,4-d][1,3,2]dioxaphosphol-4-yl}-9H-purin-6-yl)butanimidate
—— 2-amino-9-(<i>O</i><sup>2</sup>,<i>O</i><sup>3</sup>,<i>O</i><sup>5</sup>-triacetyl-ξ-<i>D</i>-xylofuranosyl)-1,9-dihydro-purin-6-one 6979-94-8 C16H19N5O8
2-amino-9-(<i>O</i><sup>2</sup>,<i>O</i><sup>3</sup>,<i>O</i><sup>5</sup>-triacetyl-ξ-<i>D</i>-xylofuranosyl)-1,9-dihydro-purin-6-one
—— 7-methyl-guanosinium 22164-16-5 C11H17N5O5
7-methyl-guanosinium
—— Adenosine 5'-triphosphate disodium salt hydrate from microbial source, min. 99% (HPLC) 34369-07-8 C10H14N5Na2O14P3-2
Adenosine 5'-triphosphate disodium salt hydrate from microbial source, min. 99% (HPLC)
—— disodium;[(1R,2R,3S,4R)-2,3-dihydroxy-4-(6-oxo-1H-purin-9-yl)cyclopentyl]methyl phosphate;hydrate 352195-40-5 C11H15N4Na2O8P
disodium;[(1R,2R,3S,4R)-2,3-dihydroxy-4-(6-oxo-1H-purin-9-yl)cyclopentyl]methyl phosphate;hydrate
—— <i>O</i><sup>2'</sup>,<i>O</i><sup>3'</sup>,<i>O</i><sup>5"</sup>-triacetyl-uridine 4105-38-8 C15H18N2O9
<i>O</i><sup>2'</sup>,<i>O</i><sup>3'</sup>,<i>O</i><sup>5"</sup>-triacetyl-uridine
—— 2-(6-Amino-2-chloro-9-purinyl)-5-(hydroxymethyl)oxolane-3,4-diol hydrate 81012-94-4 C10H14ClN5O5
2-(6-Amino-2-chloro-9-purinyl)-5-(hydroxymethyl)oxolane-3,4-diol hydrate
—— sodium 6-(6-amino-8-bromo-purin-9-yl)-2-oxido-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol 76939-46-3 C10H10BrN5NaO6P
sodium 6-(6-amino-8-bromo-purin-9-yl)-2-oxido-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol
—— (3xi)-5'-o-[(4-Methylphenyl)sulfonyl]adenosine 5135-30-8 C17H19N5O6S
(3xi)-5'-o-[(4-Methylphenyl)sulfonyl]adenosine
—— 2',3'-O-(1-Methylethylidene)adenosine 362-75-4 C13H17N5O4
2',3'-O-(1-Methylethylidene)adenosine
—— 2-(4-Amino-5-iodo-7-pyrrolo[2,3-d]pyrimidinyl)-5-(hydroxymethyl)oxolane-3,4-diol 24386-93-4 C11H13IN4O4
2-(4-Amino-5-iodo-7-pyrrolo[2,3-d]pyrimidinyl)-5-(hydroxymethyl)oxolane-3,4-diol
—— Adenosine, 3-deaza- 6736-58-9 C11H14N4O4
Adenosine, 3-deaza-
—— 2'-O-Methylguanosin 2140-71-8 C11H15N5O5
2'-O-Methylguanosin
—— 9-{5-o-[(4-Methylphenyl)sulfonyl]pentofuranosyl}-9h-purin-6-amine 55197-13-2 C17H19N5O6S
9-{5-o-[(4-Methylphenyl)sulfonyl]pentofuranosyl}-9h-purin-6-amine
—— 1-[3,4-Dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-iodo-pyrimidine-2,4-dione 1024-99-3 C9H11IN2O6
1-[3,4-Dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-iodo-pyrimidine-2,4-dione
—— 9H-Purine,8-diamino-9-beta-D-ribofuranosyl- 3868-33-5 C10H14N6O4
9H-Purine,8-diamino-9-beta-D-ribofuranosyl-
—— 5-Chloro-1-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione 2880-89-9 C9H11ClN2O6
5-Chloro-1-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
—— N4-Benzoyl-2-O-methylcytidine 52571-45-6 C17H19N3O6
N4-Benzoyl-2-O-methylcytidine
—— Β-D-Ribofuranosyl)-9-benzylamino-6-purin 4294-16-0 C17H19N5O4
Β-D-Ribofuranosyl)-9-benzylamino-6-purin
—— N-[9-[5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-3,4-dihydroxyoxolan-2-yl]purin-6-yl]benzamide 81246-82-4 C38H35N5O7
N-[9-[5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-3,4-dihydroxyoxolan-2-yl]purin-6-yl]benzamide
—— 2’-C-methyladenosine 15397-12-3 C11H15N5O4
2’-C-methyladenosine
—— Adenosine sodio-2',3'-phosphate hydrate 37063-35-7 C10H13N5NaO6P
Adenosine sodio-2',3'-phosphate hydrate