74919-31-6Relevant articles and documents
NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
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Paragraph 1173; 1174; 1177, (2018/09/08)
An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
The amination of 3-bromo-2-ethoxy-1,5-naphthyridine. A reinvestigation.
Haak, H. J. W. van den,Plas, H. C. van der
, p. 83 - 86 (2007/10/02)
The reaction of 3-bromo-2-ethoxy-1,5-naphthyridine with KNH2/NH3 was reinvestigated.The procedure, described in the literature for the preparation of the title compound does not lead to this compound but to the isomeric 3-bromo-1-ethyl-1,5-naphthyridin-2(1H)-one.Reaction of this compound with KNH2/NH3 yields 3- and 4-amino-1-ethyl-1,5-naphthyridin-2(1H)-one, the latter being the main product.The title compound was prepared on reacting 2,3-dibromo-1,5-naphthyridine with sodium ethoxide.A mixture of 3- and 4-amino-2-ethoxy-1,5-naphthyridine was obtained on amination of 3-bromo-2-ethoxy-1,5-naphthyridine.In both cases the intermediacy of the respective 3,4-didehydro compounds was proposed.