- Intermolecular 1,2-Difunctionalization of Alkenes Enabled by Fluoroamide-Directed Remote Benzyl C(sp3)-H Functionalization
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A copper-catalyzed remote benzylic C-H functionalization strategy enabling 1,2-difunctionalization of alkenes with 2-methylbenzeneamides and nucleophiles, including alcohols, indoles, pyrroles, and the intrinsic amino groups, is reported, which is charact
- Li, Jin-Heng,Li, Yang,Lu, Xin,Ouyang, Xuan-Hui,Song, Ren-Jie,Sun, Qing,Xiong, Zhi-Qiang,Zhong, Long-Jin
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supporting information
(2022/01/08)
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- A Broad-Spectrum Catalytic Amidation of Sulfonyl Fluorides and Fluorosulfates**
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A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87–99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.
- Wei, Mingjie,Liang, Dacheng,Cao, Xiaohui,Luo, Wenjun,Ma, Guojian,Liu, Zeyuan,Li, Le
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p. 7397 - 7404
(2021/02/16)
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- Copper-Catalyzed, N-Directed Csp3-H Trifluoromethylthiolation (-SCF3) and Trifluoromethylselenation (-SeCF3)
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A direct and versatile copper-catalyzed trifluoromethylthiolation and trifluoromethylselenation of primary, secondary, and tertiary aliphatic C-H bonds was developed. The reaction provides direct access to molecules containing these emerging moieties in the presence of a wide range of common functional groups and in complex molecular environments.
- Modak, Atanu,Pinter, Emily N.,Cook, Silas P.
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supporting information
p. 18405 - 18410
(2019/11/19)
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- Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor
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Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
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Page/Page column 15
(2010/01/31)
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- Antiproliferative Properties of Polyamine Analogues: A Structure-Activity Study
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A basis set of polyamine analogues was designed and synthesized.These compounds were used to initiate a systematic investigation of the role of chain length, terminal nitrogen alkyl group size, and symmetry of the methylene backbone in the antineoplastic
- Bergeron, Raymond J.,McManis, James S.,Liu, Charles Z.,Feng, Yang,Weimar, William R.,et al.
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p. 3464 - 3476
(2007/10/02)
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