Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 863548-52-1, name is (1-Methyl-1H-pyrazol-5-yl)methanamine, A new synthetic method of this compound is introduced below., category: pyrazoles-derivatives
Step a. To a mixture of tert-butyl 2-chloro-4-(3-(2-oxopyrrolidin-l-yl)phenyl)-5,7-dihydro-6H- pyrrolo[3,4-d]pyrimidine-6-carboxylate (prepared as in step a of Example 289, 0.450 g, 1.086 mmol) and l-methyl-lH-pyrazol-5-yl)methylamine (CAS Number 863548-52-1; 0.180 g, 1.629 mmol) in 1,4-dioxane (100 ml) was added K2C03 (0.450 g, 3.258 mmol) at rt. The reaction mixture was degassed for 10 min before addition of Pd2(dba)3 (0.099 g, 0.108 mmol) and Xanthphos (0.062 g, 0.108 mmol). The reaction mixture was heated at 90C for 16 h. The resulting mixture was cooled to rt, poured into water (20 ml) and extracted with EtOAc (3 x 30 ml). The combined organic phase was dried over Na2S04, filtered and concentrated under reduced pressure. The residue was purified by flash column chromatography (3.2% MeOH in DCM) yielding tert-butyl 2-(((l-methyl-lH-pyrazol-5- yl)memyl)amino)-4-(3-(2-oxopyrrolidin-l-yl)phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6- carboxylate (0.250 g, 0.511 mmol). LCMS: Method A, 1.858 min, MS: ES+ 490.41.
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; MISSION THERAPEUTICS LIMITED; GIBSON, Karl Richard; JONES, Alison; KEMP, Mark Ian; MADIN, Andrew; STOCKLEY, Martin Lee; WHITLOCK, Gavin Alistair; WOODROW, Michael D; (241 pag.)WO2017/158388; (2017); A1;,
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