1123492-82-9Relevant academic research and scientific papers
Redox deracemization of α-substituted 1,3-dihydroisobenzofurans
Chen, Xiaohan,Zhao, Ran,Liu, Ziqiang,Sun, Shutao,Ma, Yingang,Liu, Qingyun,Sun, Xia,Liu, Lei
, p. 2305 - 2308 (2021)
Chiral α-substituted 1,3-dihydroisobenzofurans are key scaffolds in a number of bioactive natural products and synthetic pharmaceuticals. However, catalytic asymmetric approaches have been rarely developed. Here, a redox deracemization technology is adopted to address the catalytic asymmetric synthesis. A broad range of α-aryl substituted 1,3-dihydroisobenzofurans are effectively deracemized in high efficiency with excellent ee. α-Alkynyl substituted ethers were also compatible with the deracemization technology.
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors
Shen, Hong C.,Ding, Fa-Xiang,Jiang, Jinlong,Verras, Andreas,Chabin, Renee M.,Xu, Suoyu,Tong, Xinchun,Chen, Qing,Xie, Dan,Lassman, Mike E.,Bhatt, Urmi R.,Garcia-Calvo, Margarita M.,Geissler, Wayne,Shen, Zhu,Murphy, Beth Ann,Gorski, Judith N.,Wiltsie, Judyann,Roy, Ranabir Sinha,Hale, Jeffrey J.,Pinto, Shirly,Shen, Dong-Ming
, p. 1550 - 1556 (2012)
A series of benzodihydroisofurans were discovered as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase (PrCP) inhibitors. The structure-activity relationship (SAR) is focused on improving PrCP activity and metabolic stability, and red
Enantioselective Transfer Hydrogenation of Oxocarbenium Ions Enables Asymmetric Access to α-Substituted 1,3-Dihydroisobenzofurans
Zhou, Likai,Jia, Kuiyong,Liu, Xigong,Liu, Lei
supporting information, p. 421 - 428 (2021/10/01)
Reported here is an efficient enantioselective transfer hydrogenation of cyclic oxocarbenium ions generated in situ through collapse of the corresponding acetal substrates. The asymmetric approach provides straightforward access to a variety of chiral α-aryl substituted 1,3-dihydroisobenzofurans in high yields with excellent enantioselectivities. α-Alkynyl substituted 1,3-dihydroisobenzofurans were also proved to be suitable substrates. In addition, when the reaction was performed at gram scale, the desired product was obtained in good yields with excellent enantioselectivity.
NOVEL SPIROPIPERIDINE PROLYLCARBOXYPEPTIDASE INHIBITORS
-
Page/Page column 47, (2011/11/13)
Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
