- Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
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One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol.
- Mete, Trimbak B.,Singh, Ankit,Bhat, Ramakrishna G.
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supporting information
p. 4709 - 4712
(2017/11/21)
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- A pyridine amide synthetic method of compound
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The invention discloses a method for synthesizing a pyridine-amide compound. The method comprises the steps of carrying out hydrolysis on a pyridine cyanogen compound shown by a formula II as a starting material in water as a solvent in the presence of an ETS-10 molecular sieve as a catalyst, heating to 100-150 DEG C, reacting until the reaction, which is tracked and detected by virtue of TLC (Thin-Layer Chromatography), is completed and carrying out post-treatment on the reaction solution to obtain the pyridine-amide compound represented by the formula I. According to the method disclosed by the invention, the ETS-10 molecular sieve is taken as a catalyst to carry out hydrolysis on pyridine cyanogen to obtain a single pyridine-amide product, the conversion rate is 100%, the yield is above 95% and the catalyst can be repeatedly used for at least 5 times.
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Paragraph 0042; 0043
(2019/02/02)
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- CXCR4 Receptor Antagonists
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Disclosed are compounds that are antagonists of the CXCR4 receptor.
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Paragraph 0141; 0142
(2013/11/06)
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- CXCR4 RECEPTOR ANTAGONISTS
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The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
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Page/Page column 38-39
(2012/05/04)
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- SOLVENT AND TEMPERATURE DEPENDENT REGIOSELECTIVE REACTIONS BETWEEN 2-CHLORO-6-CYANOPYRIDINE AND ALIPHATIC ALCOHOLS
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Reaction of 2-chloro-6-cyanopyridine with aliphatic mono- and di-alcohols or ethylene glycols affords, depending on the reaction conditions, alkoxypyridines or imino ester pyridines or a mixture of both types of compounds.It is suggested that the product distribution is determined by the stability of an imidate anion formed as an intermediate.An improved synthesis of 2-chloro-6-cyanopyridine is also described.
- Elman, Bjoern
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p. 4941 - 4948
(2007/10/02)
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