Catalytic Enantioselective Formal Synthesis of MDM2 Antagonist RG7388 and Its Analogues

Catalytic Enantioselective Formal Synthesis of MDM2 Antagonist RG7388 and Its Analogues
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MDM2拮抗剂RG7388及其类似物的催化对映选择性形式合成

DOI:
10.1002/cjoc.201900530
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发表时间:
2020-05
影响因子:
5.4
通讯作者:
Deng Wei-Ping
Deng Wei-Ping
中科院分区:
化学2区
文献类型:
--
作者:
Zou Xue-Jie;Yang Wu-Lin;Zhu Jing-Yan;Deng Wei-Ping

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Summary of main observation and conclusionThe catalytic asymmetric 1,3‐dipolar [3 + 2] cycloaddition of azomethine ylides with stilbenes has been established, affording structurally diverse pyrrolidines bearing four contiguous stereocenters with stereo‐diversity in generally high yields and good to excellent stereoselectivities (up to 98% yield, 99 : 1 dr, >99% ee).Meanwhile, this strategy allowed the formal synthesis of antitumor drug RG7388 (Phase III clinical study) and its analogues in high efficiency.
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