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Practical Synthesis of (2′R)-2′-Deoxy-2′-C-methyluridine by Highly Diastereoselective Homogeneous Hydrogenation
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2010-12-06 00:00:00 , DOI: 10.1021/jo101822j
Sébastien Lemaire 1 , Ioannis Houpis 1 , Rainer Wechselberger 1 , Jaak Langens 1 , Wim A. A. Vermeulen 1 , Nico Smets 1 , Ulrike Nettekoven 2 , Youchu Wang 3 , Tingting Xiao 3 , Haisheng Qu 3 , Renmao Liu 3 , Tim H.M. Jonckers 4 , Pierre Raboisson 4 , Koen Vandyck 4 , Karl M. Nilsson 5 , Vittorio Farina 1
Affiliation  

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.

中文翻译:

(2'实用合成- [R)-2'-脱氧-2'- Ç -methyluridine由高度非对映均相氢化

2'-脱氧-2'--亚甲基尿苷的非对映选择性氢化是在均相条件下使用低负载量的手性Rh催化剂进行的。这与底物合成的改进相结合,使得能够以大于10 kg的规模顺利地中试制备标题化合物。
更新日期:2010-12-06
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