5'-DMT-2'-氟-苯甲酰基-2'-脱氧腺苷

5'-DMT-2'-氟-苯甲酰基-2'-脱氧腺苷性质、用途与生产工艺

概述

生产方法 

40615-36-9

136834-20-3

136834-21-4

将N-(9-((2R,3R,4R,5R)-3-氟-4-羟基-5-(羟甲基)四氢呋喃-2-基)-9H-嘌呤-6-基)苯甲酰胺（570g，1.53mol）溶解于吡啶（2.85L，35.2mol）中。将反应混合物冷却至2.6℃，随后加入4,4'-双甲氧基三苯甲基氯（543g，1.60mol）。在0至5℃下搅拌反应混合物2小时，然后缓慢升温至室温。通过LC/MS监测反应进程，确认反应完全后，将混合物冷却至5℃以下，缓慢加入甲醇（124ml，3.05mol）淬灭反应，持续搅拌15分钟。随后，将反应混合物与甲苯（2.00L）共蒸发浓缩，再用乙酸乙酯（2.85L）和正庚烷（2.85L）的混合溶剂稀释。用9%的饱和碳酸氢钠水溶液（2.0L）洗涤有机层，再加入乙酸乙酯（2.85L）以确保粗产物完全溶解。搅拌5分钟后，分离有机层和水层。有机层用水（2.0L）洗涤后，开始有固体缓慢析出。分离水层后，将有机层浓缩至约原体积的1/50。粗产物用正庚烷（2.00L）和甲苯（0.50L）的混合溶剂浆化，搅拌15分钟后，通过真空过滤收集浅黄色固体。滤饼依次用（1）正庚烷（0.60L）和甲苯（0.30L）的混合溶剂及（2）正庚烷（3.00L）洗涤。固体在室温下干燥30分钟后，转移至托盘，于50℃真空烘箱中干燥过夜，得到目标化合物N-(9-((2R,3R,4R,5R)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-3-氟-4-羟基四氢呋喃-2-基)-9H-嘌呤-6-基)苯甲酰胺（996.7g，1.47mol，产率97%）。NMR数据确认产物结构。

参考文献：

[1] Patent: WO2018/152450, 2018, A1. Location in patent: Page/Page column 61; 62

[2] Bioorganic and Medicinal Chemistry Letters, 2010, vol. 20, # 15, p. 4539 - 4543

[3] Patent: WO2018/156625, 2018, A1. Location in patent: Paragraph 0290; 0291

[4] Journal of Medicinal Chemistry, 1993, vol. 36, # 7, p. 831 - 841

[5] Tetrahedron Letters, 1998, vol. 39, # 13, p. 1657 - 1660

5'-DMT-2'-氟-苯甲酰基-2'-脱氧腺苷 上下游产品信息

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5'-DMT-2'-氟-苯甲酰基-2'-脱氧腺苷 生产厂家

136834-21-4, 5'-DMT-2'-氟-苯甲酰基-2'-脱氧腺苷 相关搜索:

• Modified（deoxy）nucleoside
• 化工中间体
• 医用原料
• 抑制剂
• 保护核苷
• 中间体-DMT-2'-F Protected Nucleosides
• 高端化学
• N6-苯甲酰基-5'-O-[双(4-甲氧基苯基)苯甲基]-2'-氟-2'-脱氧腺苷
• 化合物 DMT-2'-F-BZ-DA
• N6-苯甲酰-2'-脱氧-5'-O-二甲基色胺-2'-氟腺苷
• 5'-O-DMT-2'-氟-N6-苯甲酰基脱氧腺苷
• N-[9-[(2R,3R,4R,5R)-5-[[双(4-甲氧基苯基)(苯基)甲氧基]甲基]-3-氟-4-羟基-2-四氢呋喃基]-9H-嘌呤-6-基]苯甲酰胺
• N6-苯甲酰基-5'-O-DMT-2'-氟-脱氧腺苷 英文名称:
• N6-苯甲酰基-2'-脱氧-2'-氟-5'-O-(4,4'-二甲氧基三苯甲基)腺苷
• N6-苯甲酰基-2-脱氧-5-O-DMT-2-氟腺苷酸
• N-苯甲酰基-5'-O-[双(4-甲氧基苯基)苯甲基]-2'-脱氧-2'-氟腺苷
• N-(9-((2R,3R,4R,5R)-5-((BIS(4-METHOXYPHENYL)(PHENYL)METHOXY)METHYL)-3-FLUORO-4-HYDROXYTETRAHYDROFURAN-2-YL)-9H-PURIN-6-YL)BENZAMIDE
• 5'-DMT-2'-氟-苯甲酰基-2'-脱氧腺苷
• N-(9-((2R,3R,4R,5R)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-3-氟-4-羟基四氢呋喃-2-基)-9H-嘌呤-6-基)苯甲酰胺
• N-苯甲酰基-5'-O-[二(4-甲氧基苯基)苯基甲基]-2'-脱氧-2'-氟腺苷
• 5'-O-(4,4'-二甲氧基三苯甲基)-N6-苯甲酰基-2'-氟脱氧腺苷
• 136834-21-4
• N6-Bz-5'-O-DMT-2'-F-dA N6-Benzoyl-5'-O-(4,4’-dimethoxytrityl)-2'-fluoro-2'-deoxy-adenosine
• 5’-O-DMT-2'-F-dA(bz)
• 5'-O-DMT-N6-BENZOYL-2'-FLUORO-2'-DEOXYADENOSINE
• N6-Benzoyl-5'-O-[bis(4-Methoxyphenyl)phenylMethyl]-2'-Fluoro-2'-Deoxyadenosine
• DMT-2'-F-Bz-A
• 5'-O-DMT-2'-F-Bz-dA
• DMT-2'-F-Bz-dA
• DMT-2'-F-A(Bz)
• N6-Benzoyl-2'-deoxy-5'-O-DMT-2'-fluoroadenosine
• 5'-O-DMTr-2'-F-dA(Bz)
• N6-Bz-2'-F-5'-O-DMT-2'-dA
• N6-Bz-DMT-2'-F-dA
• 5'-O-DMT-2'-F-N6-Bz-deoxyadenosine
• 5'-O-DMT-N6-benzoyl-2'-fluoro-2'-deoxyadenosine
• DMT-2'-F-Bz-A
• DMT-2'-F-Bz-dA
• DMT-2'-F-dA(Bz)
• 5'-ODMT-2'-Fluoro-N-Bz Adenosine
• N-[9-[(2R,3R,4R,5R)-5-[[Bis(4-methoxyphenyl)(phenyl)methoxy]methyl]-3-fluoro-4-hydroxy-2-tetrahydrofuryl]-9H-purin-6-yl]benzamide
• 5'-O-DMT-2'-F-Benzoyl-Deoxyadenosine
• 5'-O-DMT-2'-Fluoro-N6-Benzoyl-2'-deoxyadenosine
• Adenosine, N-benzoyl-5'-O-[bis(4-Methoxyphenyl)phenylMethyl]-2'-deoxy-2'-fluoro- ISO 9001：2015 REACH
• 5'-O-DMT-N6-Bz-2'-F-dA
• DMT-2'-F-BZ-DA N-(9-((2R,3R,4R,5R)-5-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-3-fluoro-4-hydroxytetrahydrofuran-2-yl)-9H-purin-6-yl)benzamide
• 5'-DMT-2'-F-Bz-dA
• AK-64782
• N6-Benzoyl-5'-O-DMT-2'-fluoro-2'-deoxyadenosine
• Adenosine, N-benzoyl-5'-O-[bis(4-Methoxyphenyl)phenylMethyl]-2'-deoxy-2'-fluoro-
• N-Benzoyl-5'-O-[bis(4-methoxyphenyl)phenylmethyl]-2'-deoxy-2'-fluoroadenosine
• N6-benzoyl-2'-deoxy-2'-fluoro-5'-O-(4,4'-dimethoxytrityl)adenosine