Exploring the Scope of Asymmetric Synthesis of β‑Hydroxy-γ-lactams via Noyori-type Reductions
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https://figshare.com/articles/dataset/Exploring_the_Scope_of_Asymmetric_Synthesis_of_Hydroxy-_-lactams_via_Noyori-type_Reductions/3848631
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资源简介：
Enantio- and diastereoselective
hydrogenation of β-keto-γ-lactams
with a ruthenium–BINAP catalyst, involving dynamic kinetic
resolution, has been employed to provide a general, asymmetric approach
to β-hydroxy-γ-lactams, a structural motif common to several
bioactive compounds. Full conversion to the desired β-hydroxy-γ-lactams
was achieved with high diastereoselectivity (up to >98% de) by
addition
of catalytic HCl and LiCl, while β-branching of the ketone substituent
demonstrated a pronounced effect on the modest to excellent enantioselectivity
(up to 97% ee) obtained.
创建时间：
2016-10-03
