Practical and scalable synthesis of a benzonitrile derivative via palladium-catalyzed cyanation with potassium ferrocyanide
A practical and reproducible synthetic method for the preparation of a benzonitrile derivative (1) from an aryl bromide (2) via Pd-catalyzed cyanation was established with dimethylacetamide (DMAc)-toluene as a mixed solvent. Optimization was examined by a design of experiments (DoE) technique to enhance reaction conversion and reduce the dimeric impurity 3, and desired benzonitrile derivative 1 was successfully obtained in high yields with excellent quality control on a 117 kg scale.
INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF
A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromo
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Page/Page column 13
(2010/10/03)
6-PYRIMIDINYL-PYRIMID-2-ONE DERIVATIVE
A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g.
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Page/Page column 10-11; 18-19
(2009/04/25)
2-SUBSTITUTED-6-HETEROCYCLIC PYRIMIDONE DERIVATIVES AS TAU PROTEIN KINASE 1 INHBITORS
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein each R1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C3
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Page/Page column 21; 25
(2008/12/07)
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