Large scale synthesis of 2'-amino-LNA thymine and 5-methylcytosine nucleosides.

作者: Andreas Stahl Madsen , Anna Søndergaard Jørgensen , Troels Bundgaard Jensen , Jesper Wengel

DOI: 10.1021/JO302036H

关键词:

摘要: Thymine intermediate 17 has been synthesized on a multigram scale (50 g, 70 mmol) from starting sugar 1 in 15 steps an overall yield of 73%, with only 5 purification steps. The key thymine 18 was obtained single step 96% yield, whereas the 5-methylcytosine 20 2 58% yield. This highly efficient large route necessitates and 3 novel to obtain N2′-functionalized amino-LNA phosphoramidites these intermediates, respectively.

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