- Nickel-Catalyzed Dearomative Arylboration of Indoles: Regioselective Synthesis of C2- And C3-Borylated Indolines
-
Indole dearomatization is an important strategy to access indolines: a motif present in a variety of natural products and biologically active molecules. Herein, a method for transition-metal catalyzed regioselective dearomative arylboration of indoles to
- Brown, M. Kevin,Crook, Phillip F.,Kuniyil, Rositha,Liu, Peng,Trammel, Grace L.
-
supporting information
p. 16502 - 16511
(2021/10/20)
-
- Design, synthesis, and biological evaluation of novel stachydrine derivatives as potent neuroprotective agents for cerebral ischemic stroke
-
Stachydrine is a natural product with multiple protective biological activities, including those involved in preventing cancer, ischemia, and cardiovascular disease. However, its use has been limited by low bioavailability and unsatisfactory efficacy. To address this problem, a series of stachydrine derivatives (A1/A2/A3/A4/B1/B2/B3/B4) were designed and synthesized, and biological studies were carried out in vitro and in vivo. When compared with stachydrine, Compound B1 exhibited better neuroprotective effects in vitro, and significantly reduced infarction size in the model of the middle cerebral artery occlusion rat model. Therefore, Compound B1 was selected for further research on ischemic stroke. [Figure not available: see fulltext.].
- Zhang, Liang,Li, Feng,Hou, Chenhui,Zhu, Sifeng,Zhong, Lili,Zhao, Jianchun,Song, Cai,Li, Wenbao
-
p. 2529 - 2542
(2020/05/25)
-
- Oxaziridine-mediated oxyamination of indoles: An approach to 3-aminoindoles and enantiomerically enriched 3-aminopyrroloindolines
-
A radical solution: A highly regioselective copper(II)-catalyzed oxyamination of N-acyl indoles with oxaziridines gave aminal products that could be converted in a single step into 3-aminoindoles and 3-aminopyrroloindolines (see scheme). When a chiral N-acyl group was used, the core fragment of some architecturally fascinating pyrroloindoline alkaloids was formed with 91% ee. Bs=benzenesulfonyl, Moc=methoxycarbonyl. Copyright
- Benkovics, Tamas,Guzei, Ilia A.,Yoon, Tehshik P.
-
supporting information; experimental part
p. 9153 - 9157
(2011/02/19)
-
- Oxo-ester mediated native chemical ligation: Concept and applications
-
A direct oxo-ester peptide ligation method has been developed. Through the use of an activated C-terminal para nitrophenyl ester (1), it is possible to achieve direct cysteine ligations (1 + 2 → 4). Peptide substrates incorporating bulky C-terminal amino acids (1) can be accommodated with high reaction efficiency. Copyright
- Wan, Qian,Chen, Jin,Yuan, Yu,Danishefskr, Samuel J.
-
supporting information; scheme or table
p. 15814 - 15816
(2009/05/16)
-
