Synthesis 2024; 56(13): 2059-2065
DOI: 10.1055/s-0043-1774861
paper

Syntheses of 7a-Substituted Pyrrolizidine Derivatives via Stereocontrolled Anionic Cyclization

Hongjun Ming
a   School of Chemistry & Chemical Engineering, Anhui University, Hefei, Anhui Province, 230601, P. R. of China
,
Darong He
b   Nature Pharmaceutical (Anhui) Co., Ltd, 4th Floor, 6# Building, 8# Huangguan Road, Anqing Hi-Tech Development District, Anqing, Anhui Province, P. R. of China
,
Shengmeng Si
b   Nature Pharmaceutical (Anhui) Co., Ltd, 4th Floor, 6# Building, 8# Huangguan Road, Anqing Hi-Tech Development District, Anqing, Anhui Province, P. R. of China
,
Chao Xu
a   School of Chemistry & Chemical Engineering, Anhui University, Hefei, Anhui Province, 230601, P. R. of China
,
Yunge Yuan
a   School of Chemistry & Chemical Engineering, Anhui University, Hefei, Anhui Province, 230601, P. R. of China
,
Xiaoran Tian
b   Nature Pharmaceutical (Anhui) Co., Ltd, 4th Floor, 6# Building, 8# Huangguan Road, Anqing Hi-Tech Development District, Anqing, Anhui Province, P. R. of China
,
Zhigang Hu
b   Nature Pharmaceutical (Anhui) Co., Ltd, 4th Floor, 6# Building, 8# Huangguan Road, Anqing Hi-Tech Development District, Anqing, Anhui Province, P. R. of China
,
Shikuo Li
a   School of Chemistry & Chemical Engineering, Anhui University, Hefei, Anhui Province, 230601, P. R. of China
,
Hui Zhang
a   School of Chemistry & Chemical Engineering, Anhui University, Hefei, Anhui Province, 230601, P. R. of China
,
Fangzhi Huang
a   School of Chemistry & Chemical Engineering, Anhui University, Hefei, Anhui Province, 230601, P. R. of China
,
Yue-Lei Chen
b   Nature Pharmaceutical (Anhui) Co., Ltd, 4th Floor, 6# Building, 8# Huangguan Road, Anqing Hi-Tech Development District, Anqing, Anhui Province, P. R. of China
› Institutsangaben
This work is supported by the National Natural Science Foundation of China (Grant Nos. 52172174, 51872002, and 21771001), the Key Research­ and Development Projects in Anhui Province (202004a07020026), and the Program of Anhui Scientific and Technical Leaders Reserve Candidates (2018RH168).


Dedicated to Prof. Dr. Jun-Da Cen on the occasion of his 60th birthday.

Abstract

Starting from inexpensive proline and epichlorohydrin, a pivotal stereocontrolled anionic cyclization reaction paves the way for a robust and adaptable methodology to produce stereoisomers of 7a-substituted pyrrolizidine derivatives. This process yields intriguing 7a-hydroxymethyl pyrrolizidine derivatives, among them valuable trans-(2-fluorohexahydro-1H-pyrrolizin-7a-yl)methanol, which is attainable through multiple steps.

Supporting Information



Publikationsverlauf

Eingereicht: 02. Februar 2024

Angenommen nach Revision: 15. April 2024

Artikel online veröffentlicht:
06. Mai 2024

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