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Practical synthesis of (2'R)-2'-deoxy-2'-C-methyluridine by highly diastereoselective homogeneous hydrogenation |
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| Authors: | Lemaire Sébastien Houpis Ioannis Wechselberger Rainer Langens Jaak Vermeulen Wim A A Smets Nico Nettekoven Ulrike Wang Youchu Xiao Tingting Qu Haisheng Liu Renmao Jonckers Tim H M Raboisson Pierre Vandyck Koen Nilsson Karl M Farina Vittorio |
| Affiliation: | Johnson and Johnson Pharmaceutical Development, Turnhoutseweg 30, B-2340 Beerse, Belgium. slemaire@its.jnj.com |
| Abstract: | Diastereoselective hydrogenation of 2'-deoxy-2'-exo-methyleneuridine was carried out under homogeneous conditions using a low loading of a chiral Rh catalyst. This, coupled with improvements in the synthesis of the substrate, allowed the smooth pilot plant preparation of the title compound on >10 kg scale. |
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