تفاعل #417915

ord-c8a0439acf424376a93f954532d0131b

معادلة التفاعل

N#N
N2
C[Si](C)(C)CCOc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1OCc1ccccc1
9-(2-O-benzyl-β-D-arabinofuranosyl)-6-[2-(trimethylsilyl)ethoxy]-9H-purine
COc1ccc(C(Cl)(c2ccccc2)c2ccc(OC)cc2)cc1
4,4′-dimethoxytrityl chloride
COc1ccc(C(OC[C@H]2O[C@@H](n3cnc4c(OCC[Si](C)(C)C)ncnc43)[C@@H](OCc3ccccc3)[C@@H]2O)(c2ccccc2)c2ccc(OC)cc2)cc1
product
المردود 44.4%
COc1ccc(C(OC[C@H]2O[C@@H](n3cnc4c(OCC[Si](C)(C)C)ncnc43)[C@@H](OCc3ccccc3)[C@@H]2O)(c2ccccc2)c2ccc(OC)cc2)cc1
9-{5-O-[bis(4-methoxyphenyl)(phenyl)methyl]-2-O-benzyl-β-D-arabinofuranosyl}-6-[2-(trimethylsilyl)ethoxy]-9H-purine
المردود 44.4%

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىquenched with 100 mL saturated NaHCO3 solution
  2. 2
    استخلاصAfter the aqueous layer was extracted with dichloromethane (100 mL) three times
  3. 3
    أخرىevaporated
  4. 4
    أخرىThe residue was purified by flash chromatography (gradient

الإجراء التجريبي

Under the protection of N2, to a solution of 9-(2-O-benzyl-β-D-arabinofuranosyl)-6-[2-(trimethylsilyl)ethoxy]-9H-purine (1.60 g, 3.49 mmol) in 20 mL pyridine was added 4,4′-dimethoxytrityl chloride (2.13 g, 6.28 mmol). The mixture was stirred at room temperature for 2 h. The reaction was diluted with 100 mL dichloromethane and quenched with 100 mL saturated NaHCO3 solution. After the aqueous layer was extracted with dichloromethane (100 mL) three times, the organic layers were combined and evaporated. The residue was purified by flash chromatography (gradient: hexane with EtOAc 0-100%, with 1% triethylamine in both hexane and EtOAc) to produce 1.18 g (1.55 mmol, 44.4%) product. LCMS: for C43H48N4O7Si calculated 760.9. found 762.5 [M+H]+. 1H NMR (600 MHz, CD3CN) δ: 8.39 (s, 1H), 8.10 (s, 1H), 7.42-7.40 (m, 2H), 7.29-7.13 (m, 10H), 6.86-6.85 (m, 2H), 6.81-6.77 (m, 4H), 6.50 (d, J=5.5 Hz, 1H), 4.69-4.65 (m, 2H), 4.49-4.45 (m, 2H), 4.24-4.21 (m, 2H), 4.02 (m, 1H), 3.8 (dd, 10.4, 6.3 Hz, 1H), 3.29 (dd, J=10.4, 3.5 Hz, 1H), 1.22 (m, 2H), 0.09 (s, 1H). 13C NMR (600 MHz, CD3CN) δ: 160.82, 152.01, 142.44, 130.24, 130.21, 128.39, 128.25, 128.01, 127.86, 127.61, 127.05, 113.21, 83.56, 82.87, 82.37, 74.31, 72.54, 65.26, 63.56, 55.10, 17.27, −2.13.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US08877439B2uspto-grants-2014_11