- Remote Directed Isocyanation of Unactivated C(sp3)-H Bonds: Forging Seven-Membered Cyclic Ureas Enabled by Copper Catalysis
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Reported herein is an unprecedented copper-catalyzed site-selective ?-C(sp3)-H bonds activation of aliphatic sulfonamides for constructing the synthetically useful seven-membered N-heterocycles. A key to success is the use of in-situ-formed amide radicals, to activate the inert C(sp3)-H bond, and inexpensive TMSNCO, as a coupling reagent under mild conditions. To the best of our knowledge, this represents the first use of alkylamine derivatives as a five-membered synthon to prepare a seven-membered N-heterocycles.
- Zhang, Hongwei,Tian, Peiyuan,Ma, Lishuang,Zhou, Yulu,Jiang, Cuiyu,Lin, Xufeng,Xiao, Xiao
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p. 997 - 1002
(2020/02/15)
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- Copper-Catalyzed Amide Radical-Directed Cyanation of Unactivated Csp3-H Bonds
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A method for site-selective intermolecular δ/?-Csp3-H cyanation of aliphatic sulfonamides is developed using TsCN as the cyanating reagent, catalyzed by a Cu(I)/phenanthroline complex. The mild, expeditious, and modular protocol allows efficient remote Csp3-H cyanation with good functional group tolerance and high regioselectivity. Mechanistic studies indicate that the reaction might proceed through a Cu(I)-mediated N-F bond cleavage to generate an amidyl radical, 1,5-HAT, and cyano group transfer of the resulting carbon radical with TsCN.
- Zhang, Hongwei,Zhou, Yulu,Tian, Peiyuan,Jiang, Cuiyu
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- Corresponding amine nitrile and method of manufacturing thereof
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The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
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Paragraph 0138; 0139; 0140; 0147; 0148
(2018/05/07)
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- N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities
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Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
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Paragraph 0470
(2014/09/30)
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- Direct catalytic formation of primary and tertiary amides from non-activated carboxylic acids, employing carbamates as amine source
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The operationally simple titanium(IV)- or zirconium(IV)-catalyzed direct amidation of non-activated carboxylic acids with ammonium carbamates generates primary, and tertiary N,N-dimethyl-substituted amides in good to excellent yields. Copyright
- Tinnis, Fredrik,Lundberg, Helena,Adolfsson, Hans
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supporting information
p. 2531 - 2536
(2012/11/06)
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- Inhibitors of protein kinases
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Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
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Page/Page column 19
(2011/10/04)
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- PRODUCTION METHOD FOR PRIMARY AMINE
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PROBLEM TO BE SOLVED: To provide a method for efficiently producing a primary amine. SOLUTION: By reacting n-hexyl acetate with ammonia in super-critical water as the reaction field, a reaction generating n-hexylamine, i.e. a reaction peculiar to super-critical water, is caused to occur. That is to say, a primary amine is generated by utilizing such a new chemical reaction that when ammonia is reacted with an acetate, a carbon atom adjacent to an ester bond is subjected to nucleophilic attack by ammonia, not by utilizing a normal-type reaction wherein the carbonyl carbon of an ester bond is subjected to the nucleophilic attack.
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Page/Page column 25; 52
(2008/06/13)
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- Mild oxidative one-carbon homologation of aldehyde to amide
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One-carbon homologation of aldehyde into amide is realized in one-pot by its reaction with potassium α-p-methoxyphenyl-α-isocyano acetic acid (1c) and hydrochloride salt of dimethylamine (3a) in toluene at room temperature followed by acidic workup. In this multicomponent reaction, 1c served as donor of the CONH2 function to aldehyde, while the dimethylamine acted as a shuttle molecule to initiate/terminate the sequence and to mediate the internal redox process of one of the three-component adducts. Ready accessibility, nominal cost of the reagents, and mild conditions are attractive features of the present method. Copyright
- Bonne, Damien,Dekhane, Mouloud,Zhu, Jieping
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p. 6926 - 6927
(2007/10/03)
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- Cycloalkylamides and their therapeutic applications
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The present invention relates to the use of compounds of formula (I) for the treatment of a variety of disorders including, but not limited to, epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, neuroprotection, and movement disorders.
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- Cycloalkylamides and their therapeutic applications
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The present invention relates to the use of compounds of formula (I) for the treatment of a variety of disorders including, but not limited to, epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, neuroprotection, and movement disorders.
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