1254473-66-9Relevant articles and documents
VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
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Paragraph 0066; 0076; 0077, (2018/06/23)
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
A chiral 1 - (3,5- two chloropyridine -4-yl)-ethanol synthesis method
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Paragraph 0020-0022, (2017/03/28)
The invention discloses an asymmetric synthesis method of 1-(3,5-dichloropyridine-4-yl)-ethanol. The asymmetric synthesis method comprises the following steps: (A) under an action of lithium amide, carrying out a reaction of 3,5-dichloropyridine (I) with acetaldehyde to generate (+/-)-1-(3,5-dichloropyridine-4-yl)-ethanol (II); (B) under an action of an oxidant, allowing (+/-)-1-(3,5-dichloropyridine-4-yl)-ethanol (II) to generate 1-(3,5-dichloropyridine-4-yl)-ethyl ketone (III); and (C) in the presence of a chiral ligand, carrying out a reaction of 1-(3,5-dichloropyridine-4-yl)-ethyl ketone with a borane reagent, and thus obtaining the 1-(3,5-dichloropyridine-4-yl)-ethanol (IV) having a single optical isomer. Compared with traditional chiral column separation of (+/-)-1-(3,5-dichloropyridine-4-yl)-ethanol, the method has the prominent advantages that: (1) the reactions are simple, the operation is easy, the total yield is high, and the optical purity is more than 98%; (2) the industrial preparation period is shortened obviously, and equipment requirements are low; and (3) the preparation cost is low, and the method is suitable for industrial production.
PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2
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Page/Page column 53, (2011/12/02)
A compound of formula la or formula lb, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; -NHR3; fused aryl-C4-7-heterocycloalkyl; - CONR4R5; -NHCO