- Convenient preparation of naphthyridines from halopyridines: Sequential Heck coupling and cyclization
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A simple method for the preparation of 1,7-naphthyridine and 1,6-naphthyridine from the corresponding aminopyridine starting materials is presented.
- Phuan, Puay-Wah,Kozlowski, Marisa C
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- A New Approach to the Preparation of 1,6- and 1,7-Naphthyridines
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Substituted 1,6- and 1,7-naphthyridines can be prepared by a simple route from readily available pyrindane; this method is more flexible and produces higher yields than previous routes.
- Giam, C. S.,Ambrozich, Deborah
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Read Online
- One-pot homo- and cross-coupling of diazanaphthalenes via C-H substitution: Synthesis of Bis- and Tris-diazanaphthalenes
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The transition metal-free coupling reactions of unactivated diazanaphthalenes were studied using only lithium tetramethylpiperidine (LiTMP) reagent. Symmetrical and nonsymmetrical bis-diazanaphthalenes were synthesized in moderate to high yield by homo- and cross-coupling of related monomers. In addition, the single-step synthesis of diquinoxalino [2,3-a: 2', 3'c] phenazine and 2,2': 3', 2″ - terquinoxaline using the appropriate equivalent amount of LiTMP was performed. The products were characterized by means of NMR spectroscopy and HRMS spectrometry.
- Ucar, Sefa,Dastan, Arif
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p. 4013 - 4022
(2020/09/21)
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- HETEROARYL COMPOUNDS AS CXCR4 INHIBITORS, COMPOSITION AND METHOD USING THE SAME
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The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the CXCR4 pathway.
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Paragraph 00305-00307
(2019/04/16)
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- Modular design of pyridine-based acyl-transfer catalysts
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Derivatives of 3,4-diaminopyridine have been synthesized and studied as catalysts for acyl-transfer reactions. The design of these catalysts is guided by the stability of their acetyl intermediates as determined through theoretical calculations at the B3LYP/6-311 + G(d,p)//B3LYP/6-31G(d) level of theory. The most promising catalysts have been synthesized through a three- to five-step synthesis starting from 3,4-diaminopyridine. The catalytic activity has been determined for the acylation of 1-ethynylcyclohexanol with acetic anhydride at 23°C and with isobutyric anhydride at 40°C. For both reactions, the catalytic activity depends dramatically on the substitution pattern of the diaminopyridines. Best results are obtained with catalysts containing alkyl substituents at both amine nitrogens. Georg Thieme Verlag Stuttgart.
- Held, Ingmar,Xu, Shangjie,Zipse, Hendrik
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p. 1185 - 1196
(2008/02/02)
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- A one-pot method for the synthesis of naphthyridines via modified friedl?nder reaction
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A one-pot method for the preparation of 1,8-naphthyridine derivatives is reported. The method involves the dimetalation of an appropriate N-2-pyridylpivalamide or tert-butylcarbamate followed by reaction with a β-dimethylamino or β-alkoxyacrolein derivative. This method is also applicable to 1,6-naphthyridines. Georg Thieme Verlag Stuttgart.
- Zhichkin, Pavel,Beer, Catherine M. Cillo,Rennells, W. Martin,Fairfax, David J.
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p. 379 - 382
(2007/10/03)
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- ARYLPIPERAZINYL-CYCLOHEXYL INDOLE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
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Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise (I) wherein: Ra, R1, R2 and R3 are each, independently, hydrogen, or a substituent selected from halogen, CF3, alkyl, alkoxy, MeSO2, amino or aminocarbonyl (each optionally substituted by one or two groups selected from alkyl and benzyl) carboxy, or alkoxycarbonyl; or two adjacent of Ra and R1-4 together can form a 5-7 membered carbocyclic or heterocyclic ring which is optionally substituted by a substituent defined above; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, arylalkyl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, alkoxy or benzyloxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is CH or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
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- General synthetic method for naphthyridines and their N-oxides containing isoquinolinic nitrogen
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Substituted naphthyridines containing isoquinolinic nitrogen were synthesized by the reaction of o-ethynylpyridinecarbaldehydes with ammonia. The synthesis of their N-oxides was also achieved by a basic cyclization reaction of the same pyridine derivatives via the corresponding oximes.
- Numata, Atsushi,Kondo, Yoshinori,Sakamoto, Takao
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p. 306 - 311
(2007/10/03)
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- Heterocycylic-substituted quinoline-carboxylic acids
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1-Substituted-6-fluoro-7-heterocyclic-1,4-dihydroquino-1-(or dihydronaphthyridin)-4-one carboxylic acids have antibacterial properties. The 7-heterocyclic group is a bicyclic group, one of the rings of which is saturated and the other ring of which is unsaturated.
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