- Photoinduced remote regioselective radical alkynylation of unactivated C-H bonds
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A method for the remote regioselective alkynylation of unactivated C(sp3)-H bonds in diverse aliphatic amides by photogenerated amidyl radicals has been developed. The site-selectivity is dominated via a 1,5-hydrogen atom transfer (HAT) process of the amide. Mild reaction conditions and high regioselectivity are demonstrated in this methodology.
- Hu, Qu-Ping,Liu, Yong-Ze,Liu, Yu-Tao,Pan, Fei
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supporting information
p. 2295 - 2298
(2022/02/25)
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- Remote Regioselective Radical C-H Functionalization of Unactivated C-H Bonds in Amides: The Synthesis of gem-Difluoroalkenes
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The site-selective functionalization of unactivated aliphatic amines is an attractive and challenging synthetic approach. We herein report a general strategy for the remote site-selective functionalization of unactivated C(sp3)-H bonds in amides by photogenerated amidyl radicals to form gem-difluoroalkenes with trifluoromethyl-substituted alkenes. The site selectivity is controlled by a 1,5-hydrogen atom transfer (HAT) process of the amide. This photocatalyzed transformation shows both chemo- and site-selectivity, facilitating the formation of a secondary, tertiary, or quaternary carbon center.
- Hu, Qu-Ping,Cheng, Jing,Wang, Ying,Shi, Jie,Wang, Bi-Qin,Hu, Ping,Zhao, Ke-Qing,Pan, Fei
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supporting information
p. 4457 - 4462
(2021/05/26)
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- NURR1 RECEPTOR MODULATORS
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Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.
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Paragraph 0646; 0996-0998
(2020/09/08)
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- Directed γ-C(sp3)-H Alkylation of Carboxylic Acid Derivatives through Visible Light Photoredox Catalysis
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Visible light photoredox catalysis enables direct γ- C(sp3)-H alkylation of saturated aliphatic carbonyl compounds. Electron-deficient alkenes are used as the coupling partners in this reaction. Distinguished site selectivity is controlled by the predominant 1,5-hydrogen atom transfer of an amidyl radical generated in situ.
- Chen, Dian-Feng,Chu, John C. K.,Rovis, Tomislav
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p. 14897 - 14900
(2017/10/31)
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- A method for preparing DL-leucine (by machine translation)
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The invention discloses a method for preparing DL-leucine. The method of the invention first through ethanol, acetamide, ethanol sodium and isobutyl bromide reaction, reaction solution distillation recovery ethanol, distillation residues hot-melt, filtering, cooling to crystallize, shall be 2-isobutyl-acetamide; and then the 2-isobutyl-acetamide react with sodium hypochlorite, reaction solution distillation recovery chcl, distillation residual the toluene-P-sulfonic acid reaction, the reaction liquid filtering, cooling to crystallize, shall be leucine paratoluene sulfonic acid; leucines toluene-P-sulfonic acid with sodium hydroxide reaction, and the re-adjustment to pH 6-6.5 DL-leucine can be obtained. The invention chemical synthetic mild reaction conditions, the low requirements for the equipment, production cycle is short, with little investment, low cost; relatively high yield, there are few by-products, can be produced in large quantities, which is beneficial for industrial; acetamide can be formed by preparing ketene dimer, easily available raw materials. (by machine translation)
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Paragraph 0009
(2017/03/14)
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- Analogs of isovaleramide, a pharmaceutical composition including the same, and a method of treating central nervous system conditions or diseases
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An isovaleramide analog having at least one of an increased potency, an increased half-life, and an increased stability compared to isovaleramide. The isovaleramide analog is a cyclic analog or a noncyclic analog. The isovaleramide analog is formulated into a pharmaceutical composition. A method of treating a central nervous system condition or disease is also disclosed. The method comprises administering an isovaleramide analog to a patient suffering from the central nervous system condition or disease.
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Page/Page column 7
(2010/02/15)
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- Ultrasound in organic syntheses. 19. Further studies on the conjugate additions to electron deficient olefins in aqeuous media
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Alkyl halides add smoothly to a variety of olefinic bonds conjugated with electron withdrawing groups, in the presence of zinc-copper couple. Sonication enhances the efficiency of the process, which takes place in aqeuous media following, most probably, a radical pathway.
- Dupuy,Petrier,Sarandeses,Luche
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p. 643 - 651
(2007/10/02)
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- COMPETITIVE TYPE II ELIMINATIONS IN ALIPHATIC IMIDES
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Aliphatic imides have been shown to undergo type II eliminations across the imide moiety in addition to those on the C-alkyl chain and α cleavage reactions.
- Mazzocchi, Paul H.,Jameson, William,Nishiyama, Tomikiro,DeCamp, Ann
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p. 989 - 992
(2007/10/02)
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