211308-81-5Relevant academic research and scientific papers
2 - Amino - 3 - iodo - 5 - chloro pyridine synthesis method
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Paragraph 0017-0031, (2018/03/13)
The invention relates to a method for synthesizing 2-amino-3-iodo-5-chloropyridine. The method comprises the steps of enabling 2-amino-5-chloropyridine and N-iodo succinimide, which serve as raw materials and are in the mass ratio of 1: (1.5-4.5), to react at the temperature of 10-102 DEG C in a proper solvent, so as to produce 2-amino-3-iodo-5-chloropyridine, and purifying, thereby obtaining a pure product 2-amino-3-iodo-5-chloropyridine. According to the method, the raw materials are relatively easily obtained and are reasonable in price; meanwhile, during preparation reaction, no heavy metal and corrosive gas are used, the reaction is mild, no special requirements on reaction equipment are required, and ordinary corrosion-resistant equipment can be applied to production; in addition, reaction conditions of the method are moderate.
HETEROARYLS AND USES THEREOF
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Paragraph 00395, (2015/08/03)
The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
HETEROARYLS AND USES THEREOF
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Paragraph 0547-0548, (2015/09/22)
The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
The acid-catalysed synthesis of 7-azaindoles from 3-alkynyl-2- aminopyridines and their antimicrobial activity
Leboho, Tlabo C.,Van Vuuren, Sandy F.,Michael, Joseph P.,De Koning, Charles B.
, p. 307 - 315 (2014/01/06)
The synthesis of 7-azaindoles from 3-alkynyl-2-aminopyridines using acidic conditions, namely, a mixture of trifluoroacetic acid (TFA) and trifluoroacetic anhydride (TFAA), is described. This methodology resulted in the synthesis of fifteen 7-azaindoles, with most containing substituents at the 2- and 5-positions. The majority of these were tested for antimicrobial activity against a range of bacteria and yeasts. The 7-azaindoles displayed the best activity against the yeasts, particularly against Cryptococcus neoformans, where activities as low as 3.9 μg ml-1 were observed.
NOVEL FURANONE DERIVATIVE
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Paragraph 0074; 0075, (2014/02/16)
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon grou
NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Paragraph 0700-0701, (2013/10/22)
This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
Practical synthesis of indoles and benzofurans in water using a heterogeneous bimetallic catalyst
Rossy, Cybille,Fouquet, Eric,Felpin, Francois-Xavier
supporting information, p. 1426 - 1431 (2013/08/23)
This paper describes the preparation of indoles, azaindoles and benzofurans in pure water by using a new heterogeneous Pd-Cu/C catalyst through a cascade Sonogashira alkynylation-cyclization sequence. Details of the optimization studies and the substrate scope are discussed. This procedure allows the preparation of heterocycles with good yields and is tolerant to a wide variety of functional groups.
Aurora isoform selectivity: Design and synthesis of imidazo[4,5- B ]pyridine derivatives as highly selective inhibitors of aurora-A kinase in cells
Bavetsias, Vassilios,Faisal, Amir,Crumpler, Simon,Brown, Nathan,Kosmopoulou, Magda,Joshi, Amar,Atrash, Butrus,Pérez-Fuertes, Yolanda,Schmitt, Jessica A.,Boxall, Katherine J.,Burke, Rosemary,Sun, Chongbo,Avery, Sian,Bush, Katherine,Henley, Alan,Raynaud, Florence I.,Workman, Paul,Bayliss, Richard,Linardopoulos, Spiros,Blagg, Julian
supporting information, p. 9122 - 9135 (2014/01/06)
Aurora-A differs from Aurora-B/C at three positions in the ATP-binding pocket (L215, T217, and R220). Exploiting these differences, crystal structures of ligand-Aurora protein interactions formed the basis of a design principle for imidazo[4,5-b]pyridine-
NOVEL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Paragraph 0532-0533; 0556-0557, (2013/11/06)
This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.
