20348-21-4Relevant articles and documents
Preparation method of fostamatinib key intermediate and intermediate thereof and method for preparing fostamatinib with intermediate
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Paragraph 0053-0064, (2019/07/04)
The invention discloses a preparation method of a fostamatinib key intermediate and an intermediate thereof and a method for preparing fostamatinib with the intermediate. The preparation method of thefostamatinib key intermediate comprises the following steps: carrying out a nucleophilic substitution reaction on a compound (2) and a compound (3) so as to obtain a fostamatinib key intermediate compound (4), and carrying out reduction cyclization on the compound (4), thereby obtaining a fostamatinib key intermediate compound (1), wherein the reaction formula is as shown in the specification. The preparation method disclosed by the invention is easy in raw material and reagent obtaining, low in price, low in cost and easy in industrialization and has the advantages of being high in synthesisyield, good in product purity, and the like.
ALKYLIDINE SUBSTITUTED HETEROCYCLYL DERIVATIVES AS ANTI-BACTERIAL AGENTS
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Page/Page column 22, (2015/06/03)
The present invention relates to alkylidine substituted heterocyclyl derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors; I in which P, Q, Ri, R2, R3 and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.