Reference of 126053-15-4, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 126053-15-4 as follows.
A mixture of intermediate 4 (0.0002 mol) and 4-chloro-6,7-dihydro-5/-/- cyclopenta[b]pyridin-7-ol (0.0002 mol) in HCI/dioxane 4N (14mul), CH3CN (1 ml) and EtOH (0.5ml) was stirred at 65C for 18 hours. HCI (0.2eq) and dioxane 4N (14mul) were added. The mixture was stirred at 65C for 18 hours, then cooled to room temperature, diluted in CH2CI2 and washed with K2CO3 10% aqueous solution. The organic layer was separated, dried (MgSO4), filtered and the solvent was evaporated till dryness. The residue (0.14g) was purified by column chromatography over Sunfire (eluent: CH2CI2/CH3OH/NH4OH 100/0/0 to 92/8/0.8; 5mum). The pure fractions were collected and the solvent was evaporated. The residue (0.072g, 50%) was crystallized from CH3CN. The precipitate was filtered off and dried, yielding 0.049g (30%) of compound 5 (M. P.: 178C).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,126053-15-4, its application will become more common.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; WO2009/37308; (2009); A1;,
Pyridine – Wikipedia,
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