Related Products of 1192-21-8, These common heterocyclic compound, 1192-21-8, name is 1-Methyl-1H-pyrazol-5-amine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Step 3 Under an atmosphere of nitrogen 1-methyl-1H-pyrazol-5-amine (284.5 mg, 2.93 mmol) was dissolved in THF (17.8 mL) at RT and treated with 1.0M LiHMDS in THF (5.86 mL, 5.86 mmol). The reaction was stirred vigorously for 10 min, and then 90 (280 mg, 1.4647 mmol) was added as a solid in one portion. The 100 mL round bottom reaction flask was equipped with a water cooled condenser and heated to 80° C. The reaction was 30percent complete after 3.5 h, so additional 1.0M LiHMDS was added (8.86 mL, total: 14.72 mL, 14.72 mmol), and the reaction heated at 80° C. for another 2.5 hours (total time at 80° C.=6 h). The reaction mixture was diluted with water (20 mL), transferred to a separatory funnel and washed with DCM (4*30 mL). The DCM washings were combined, and the aqueous layer was neutralized via the addition 1.26 mL of 11.6 M aqueous HCl. The resulting precipitate was collected via vacuum filtration to afford 373 mg (94percent) of 3-(1-methyl-1H-pyrazol-5-ylamino)isoquinoline-6-carboxylic acid (92), which was used without any further purification.
Statistics shows that 1-Methyl-1H-pyrazol-5-amine is playing an increasingly important role. we look forward to future research findings about 1192-21-8.
Reference:
Patent; Genentech, Inc.; Array BioPharma Inc.; Blake, Jim; Chen, Huifen; Chicarelli, Mark; Gaudino, John; Gazzard, Lewis; Kintz, Sam; Mohr, Pete; Robarge, Kirk; Schwarz, Jacob; Zhou, Aihe; US2014/66453; (2014); A1;,
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