161117-83-5Relevant articles and documents
Synthesis method of 8-chloro-1, 7-naphthyridine-3-formaldehyde
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Paragraph 0033-0037; 0063-0067, (2020/04/17)
The invention discloses a synthesis method of 8-chloro-1, 7-naphthyridine-3-formaldehyde, which comprises the following synthesis steps: 1) taking a compound I 2-methoxy-3-aminopyridine as an initialraw material, protecting amino to obtain a compound II; 2) reacting the compound II with an hydroformylation reagent under an alkaline condition to obtain a compound III; 3) deprotecting the compoundIII under an acidic condition to obtain a compound IV or a salt of the compound IV; 4) performing cyclization reaction on the compound IV and an acrylate compound under the action of a Lewis acid to prepare a compound V; 5) carrying out chlorination reaction on the compound V and a chlorination reagent to prepare a compound VI; and 6) dissolving the compound VI 8-chloro-1, 7-naphthyridine-3-formate as a raw material in a solvent, and reducing under the action of a reducing reagent to directly obtain 8-chloro-1, 7-naphthyridine-3-formaldehyde, namely a compound VII. The preparation method disclosed by the invention has the characteristics of suitability for industrial production, relatively low cost and simple operation.
Preparation of azaindolines and benzoyl substituted azaindolines: Precursors of triazabenzo[cd]azulen-9-one PDE4 inhibitors
Badland, Matthew,Devillers, Ingrid,Durand, Corinne,Fasquelle, Véronique,Gaudillire, Bernard,Jacobelli, Henry,Manage, Ajith C.,Pevet, Isabelle,Puaud, Jocelyne,Shorter, Anthony J.,Wrigglesworth, Roger
supporting information; experimental part, p. 5292 - 5296 (2011/10/30)
The syntheses of various substituted azaindolines are described. Azaindolines were identified as potential key intermediates towards new PDE4 inhibitors.
QUINAZOLINE DERIVATIVE
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Page/Page column 75, (2010/11/25)
This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R 1 represents a lower alkyl group et al; R 2 and R 3 are same and different and represents hydrogen atm et al; R 4 represents the substituent of the formula (II) et al; X 1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.