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An enzymatically cleavable ester functionality was readily introduced in proximity to the C4 stereogenic center at N3 by hydroxymethylation with formaldehyde, followed by standard acetylation with acetyl chloride. The resulting N3-acetoxymethyl activated DHPM (rac)-6 was obtained in ca. 80% overall yield and high purity from 4 as a single regioisomer (no N1- or bis-functionalized products could be detected). |
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谢楼上 5楼2010-09-27 12:22:44