tert-butyl3-(4-nitro-1H-pyrazol-1-yl)azetidine-1-carboxylate synthesis
- Product Name:tert-butyl3-(4-nitro-1H-pyrazol-1-yl)azetidine-1-carboxylate
- CAS Number:1314987-79-5
- Molecular formula:C11H16N4O4
- Molecular Weight:268.27
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Yield:1314987-79-5 93%
Reaction Conditions:
with caesium carbonate in N,N-dimethyl-formamide at 90; for 12 h;
Steps:
30.1 Step 1: Synthesis of tert-butyl-3-(4-nitro-1H-pyrazol-1-yl)azetidin-1-carboxylate
4-Nitro-1H-pyrazole (2.9 g, 25.77 mmol) was dissolved in DMF (30 ml). Cs2CO3 (17.6 g, 2.0 eq.) and tert-butyl-3-(methylsulfonyloxy)azetidin-1-carboxylate (6.8 g, 1.05 eq., Intermediate 21) were added thereto, followed by stirring thereof at 90°C for 12 hours. Water was added thereto to terminate the reaction. It was extracted three times with ethyl acetate, dried over MgSO4, and concentrated. It was subjected to column chromatography (MeOH:MC = 1:40) to obtain 6.45 g of the target compound in yellow color (yield: 93%). MS (ESI) m/z : 268.9 [M+H]+; 1H NMR (300 MHz, CDCl3) δ 8.30 (s, 1H), 8.14 (s, 1H), 5.09-5.03 (m, 1H), 4.44-4.29 (m, 4H), 1.46 (s, 9H).
References:
EP3722298,2020,A1 Location in patent:Paragraph 0147
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