- Radical Cyclization of Olefinic Amides through α-C(sp 3)-H Functionalization of Ketones under Catalyst-, Ligand-, and Base-Free Conditions
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A new, efficient, and practical radical cyclization of olefinic amides with ketones through α-C(sp 3)-H functionalization in the presence of tert -butyl peroxybenzoate (TBPB) is described for the first time. This protocol assembles a wide range of pivotal and useful benzoxazines in good to excellent yields under mild, catalyst-free, ligand-free, and base-free conditions with wide functional group tolerance. Moreover, the mechanistic study indicates that the α-carbonyl radical is involved in this transformation.
- Qin, Fu-Hua,Kang, Qing-Qing,Zhang, Jun-Yao,Hu, Sen-Jie,Liu, Yi,Ruan, Yiping,Zheng, Hongxing,Fang, Yi-Lin,Liu, Hongxin,Wei, Wen-Ting
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supporting information
p. 905 - 912
(2021/04/27)
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- Bioactive 3,4,5-substituted benzodiazepine 2-one drug molecules and preparation method thereof
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The invention discloses bioactive 3,4,5-substituted benzodiazepine 2-one drug molecules and a preparation method thereof and belongs to the technical field of drug synthesis. The technical scheme is characterized in that the structure of the compounds is shown in the description, wherein R1 is methyl, pyridyl, phenyl or isopropyl; R1 and R2 are selected from methyl, ethyl or phenyl independently respectively. Compared with the prior art, the compounds and the preparation method have the following beneficial effects: the synthesis method is simple, the molecular structure is novel, and the compounds have an inhibition effect on the leukemia cell line K562 and the breast cancer cell MCF-7 and are expected to be further popularized and applied.
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Paragraph 0029; 0030
(2018/04/26)
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- N-Bu4NI-catalyzed selective dual amination of sp3 C-H bonds: Oxidative domino synthesis of imidazo[1,5-c]quinazolines on a gram-scale
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An n-Bu4NI catalyzed domino reaction that involves selective dual amination of sp3 C-H bonds has been developed. The protocol affords a facile and efficient approach to the synthesis of imidazo[1,5-c] quinazolines under mild conditions.
- Zhao, Dan,Wang, Teng,Shen, Qi,Li, Jian-Xin
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supporting information
p. 4302 - 4304
(2014/04/17)
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- Trifluoromethyl-promoted homocamptothecins: Synthesis and biological activity
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The homocamptothecin (hCPT) represents a new class of topoisomerase inhibitor which combines enhanced plasma stability and strong antitumor activity. Fluorine imparts desirable characteristics to drugs by modulating both the pharmacokinetics and pharmacodynamic properties of a drug. Therefore, in an attempt to improve the antitumor activity of homocamptothecins, seven new 7-trifluoromethylated homocamptothecin derivatives were prepared by proline-catalyzed Friedlander annulation. The antitumor activity in vitro and in vivo on cancer cell lines, and inhibitory properties of topoisomerase I-mediated DNA cleavage of compounds 6c and 8b were evaluated. Several of these trifluoromethylated hCPT derivatives (such as 6a, 6b and 6c) possessed higher in vitro antitumor activity than topotecan (TPT). Especially, the compound 6c showed effective in vivo antitumor activity comparable to that of TPT.
- Zhu, Lingjian,Miao, Zhenyuan,Sheng, Chunquan,Guo, Wei,Yao, Jianzhong,Liu, Wenfeng,Che, Xiaoying,Wang, Wenya,Cheng, Pengfei,Zhang, Wannian
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experimental part
p. 2726 - 2732
(2010/08/07)
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- The reaction of o-amino aryl carboxylic acids with Grignard reagents. The unusual effect of the N-protecting group on aryl ketone formation
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The addition of Grignard reagents to the o-amino aryl carboxylic acids without any additive forms the tertiary carbinol as a major product. Unexpectedly, the aryl ketones are formed as the only isolated product if o-amino moiety of anthranilic acids is protected with Boc, trifluoroacetyl, and pivaloyl protecting groups.
- Zhang, Puwen,Terefenko, Eugene A.,Slavin, Joseph
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p. 2097 - 2099
(2007/10/03)
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