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ChemicalBook CAS DataBase List 1H-Pyrazolo[4,3-d]pyriMidine, 5-chloro-

1H-Pyrazolo[4,3-d]pyriMidine, 5-chloro- synthesis

7synthesis methods
-

Yield:633328-98-0 93%

Reaction Conditions:

with hydrogenchloride in tetrahydrofuran;water at 50; for 0.5 h;Reflux;

Steps:

c) 5-Chloro-1H-pyrazolo[4,3-d]pyrimidine
To a stirred solution of 1-(5-chloro-pyrazolo[4,3-d]pyrimidin-1-yl)-ethanone (1.5 g, 7.65 mmol) in THF (15 mL) was added 8% aqueous HC1 (14.46 mL) at 50°C and reaction mixture was refluxed for 30 mm. After completion of the reaction, it was cooled to 25°C and was extractedwith EtOAc (2xSOmL). The combined organic layers were dried over Na2504, filtered and concentrated under reduced pressure to yield the title compound as an off-white solid (1.1 g, 93%). MS (ESI): mlz = 153.0 [M-H].

References:

F. HOFFMANN-LA ROCHE AG;HOFFMANN-LA ROCHE INC.;BUETTELMANN, Bernd;KOCER, Buelent;KUHN, Bernd;PRUNOTTO, Marco;RICHTER, Hans;RITTER, Martin WO2017/137334, 2017, A1 Location in patent:Page/Page column 123; 124

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