- PREPARATION METHOD FOR DEUTERATED MACROCYCLIC COMPOUND
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Provided are a compound as represented by formula (D) and a preparation method therefor, where X2 is a halogen, Pg is selected from H and an amino protecting group, such as Cbz, Boc, Fmoc, Alloc, Teoc, methoxycarbonyl or ethoxycarbonyl. Also pr
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- Electrochemical, Iodine-Mediated α-CH Amination of Ketones by Umpolung of Silyl Enol Ethers
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The electrochemical, oxidative Umpolung reaction of silyl enol ethers utilizing simple iodide salts for the synthesis of α-amino ketones is described. The products were isolated in excellent yields of up to 100percent, and various functionalized starting materials were accepted in an undivided electrochemical cell design. Moreover, a sensitivity assessment to ensure an improved reproducibility of the reaction and cyclic voltammetry experiments were performed to postulate a plausible reaction mechanism on their basis.
- Strehl, Julia,Hilt, Gerhard
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supporting information
p. 5968 - 5972
(2020/08/12)
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- SOLID FORMS OF A MACROCYCLIC KINASE INHIBITOR
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This invention relates to crystalline solvates of (10R)-7-amino-12-fluoro-2,10,16- trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benz- oxadiazacyclotetradecine-3-carbonitrile, useful in the treatment of abnormal cell growt
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Page/Page column 33-34
(2015/01/16)
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- Novel, Acyclically Substituted Furopyrimidine Derivatives and Use Thereof
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The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
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Page/Page column 32
(2009/12/28)
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- Total Synthesis of 2,6-Dimethylergolin-8α-amines
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A stereoselective total synthesis of the racemic form of the 2,6-dimethylergolin-8α-amine derivative III, previously obtained semi-synthetically from lysergic acid, is described. Starting from the commercially available tricyclic lactam 1, the 9,10-didehy
- Waldvogel, Erwin,Engeli, Peter,Kuesters, Ernst
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p. 2084 - 2099
(2007/10/03)
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- A convenient synthesis of 4-substituted 1,2,3,4-tetrahydroisoquinolin-4-ols by a novel intramolecular Barbier reaction and by an insertion reaction: Reaction scope and limitations
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4-Substituted 1,2,3,4-tetrahydroisoquinolin-4-ols were prepared from N-(2-iodobenzyl)phenacylamines by an intramolecular Barbier reaction with butyllithium and by an insertion reaction with zerovalent nickel. The scope and limitations of these reactions were discussed.
- Kihara, Masaru,Kashimoto, Minoru,Kobayashi, Yoshimaro
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- Trisubstituted (Stannylmethyl)lithium as a Methylene Double Anion Equivalent. Reaction with Esters
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Trisubstituted (stannylmethyl)lithium reacts with electrophiles as a methylene double anion equivalent to produce enolates from esters.The reaction mechanism is discussed.
- Sato, Tadashi,Matsuoka, Hiroharu,Igarashi, Tsutomu,Minomura, Masafumi,Murayama, Eigoro
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p. 1207 - 1212
(2007/10/02)
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- Synthesis and Properties of Cyclic Keto Alkenylammonium Salts
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The cyclic keto alkenylammonium salts (4)-(8) have been prepared by a short, general route and their acidic and electrophilic properties examined.
- Jung, Michael E.,Love, Brian E.
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p. 1288 - 1290
(2007/10/02)
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- 2-(Chloromethyl)-3,5-dioxahex-1-ene. An Effective Acetonylating Reagent
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By β-elimination of 2-chloro-1-(chloromethyl)ethyl methoxymethyl ether (1) under solid-liquid phase-transfer catalytic conditions, 2-(chloromethyl)-3,5-dioxahex-1-ene (2) of high purity was readily obtained in 85percent.Allyl chloride (2) is found to be stable at ambient conditions and to be a superior reagent as CH3COCH2+ synthon for converting active proton-containing compounds such as carboxylic acids, amines, phenols, alcohols, thiols, malonate, β-diketones, β-keto esters, phenylacetonitrile, fluorene, and indene to the corresponding acetonyl derivatives in good to excellent yields (61-93percent), usually under phase-transfer catalytic conditions or in a t-BuONa-t-BuOH system.
- Gu, Xue-Ping,Nishida, Nobuyuki,Ikeda, Isao,Okahara, Mitsuo
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p. 3192 - 3196
(2007/10/02)
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- Specific Enolates from α-Amino Ketones
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The enolization of 11 tertiary α-amino ketones was investigated under three different conditions (kinetic base, thermodynamic base, thermodynamic acid) to determine the directionality of such enolates for application to alkaloid synthesis.The ketone structural variables examined were the geometry of the amine nitrogen lone pair-carbonyl array and the electronic nature of the nitrogen substituent.With the exception of 3-pyrrolidinones, increasing the electron-withdrawing nature of the nitrogen increases the amount of enolization toward nitrogen (3, 6, and 9 or 21, 24, and 27).N-Alkyl-substituted amino ketones (3, 12, 21, 33) under kinetic base conditions yield enolate distributions similar to those of the corresponding all-carbon compounds.N-Carbamato-substituted amino ketones (6, 24, 27, 30) enolize predominantly toward nitrogen under all conditions.The 3-pyrrolidinones 12, 15, and 18 afford enolates away from nitrogen under all conditions.
- Garst, Michael E.,Bonfiglio, John N.,Grudoski, David A.,Marks, Jeffrey
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p. 2307 - 2315
(2007/10/02)
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