Related Products of 152120-54-2, These common heterocyclic compound, 152120-54-2, name is tert-Butyl (((tert-butoxycarbonyl)amino)(1H-pyrazol-1-yl)methylene)carbamate, 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.
N,NDi-Boc-1H-pyrazole-1-carboxamidine (500.0 mg, 1.61 mmol) was dissolved in THE dry (6.2 mL). Then Triphenylphosphine (631.4 mg, 2.41 mmol) andHydroxymethyl-cyclopropane (150.5 mg, 2.09 mmol) were added. The reaction mixture was cooled at 0 C and Diisoporpyl azodicarboxylate (0.47 mL, 2.41 mmol) was added dropwise. The temperature was increased to 70 C and the reaction mixture was stirred at reflux 1 2h. The reaction mixture was concentrated and then diluted with DCM and H20. The aqueous phase was extracted for three times with DCM; the organicphases were collected, washed with brine twice and dried over Na2504. Solvent was removed in vacuum. The crude product was purified with chromatography column in silica gel (eluent: Petroleum Ether/AcOEt 9:1) to afford compound 24 as a yellow oil (yield 82%). 1H NMR (CDCI3) O (ppm): 0.45 (d, 2H, J = 4.8 Hz); 0.49 (d, 2H, J = 5.6Hz); 1.27 (s, 9H); 1.49 (s, 9H); 1.54 (s, 1H); 3.60 (d, 2H, J = 6.8 Hz); 6.41 (t, 1H, J =2.2 Hz); 7.69 (d, 1 H, J = 1 .2 Hz); 7.95 (s, 1 H).LCMS m/z (ES+) = 387.1 [M + Na]
Statistics shows that tert-Butyl (((tert-butoxycarbonyl)amino)(1H-pyrazol-1-yl)methylene)carbamate is playing an increasingly important role. we look forward to future research findings about 152120-54-2.
Reference:
Patent; LEAD DISCOVERY SIENA S.R.L.; BOTTA, Maurizio; MACCARI, Giorgio; SANFILIPPO, Stefania; DE LUCA, Filomena; DOCQUIER, Jean-Denis; DEODATO, Davide; (56 pag.)WO2016/55644; (2016); A1;,
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