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| | Boc-D-Azetidine-2-carboxylic acid Basic information |
| Product Name: | Boc-D-Azetidine-2-carboxylic acid | | Synonyms: | (R)-Azetidine-1,2-dicarboxylic acid 1-tert-butyl ester;(R)-1-Boc-azetidine-2-car...;1-Boc-D-azetidine-2-carboxylic acid;(R)-N-Boc-azetodome carboxylic;(R)-N-tert-Butoxycarbonylazetidine-2-carboxylic acid;(R)-1-(tert-butoxycarbonyl)azetidine-2-carboxylic acid;(R)-1-Boc-azetidine-2-carboxylic acid;Boc-(R)-azetidine-2-carboxylic acid | | CAS: | 228857-58-7 | | MF: | C9H15NO4 | | MW: | 201.22 | | EINECS: | | | Product Categories: | | | Mol File: | 228857-58-7.mol |  |
| | Boc-D-Azetidine-2-carboxylic acid Chemical Properties |
| Boiling point | 321.0±35.0 °C(Predicted) | | density | 1.246 | | storage temp. | 2-8°C | | pka | 4.01±0.20(Predicted) |
| | Boc-D-Azetidine-2-carboxylic acid Usage And Synthesis |
| Chemical Properties | White powder | | Uses | 1,2-Azetidinedicarboxylic Acid 1-(1,1-Dimethylethyl) Ester, is an useful intermediate in the synthesis of pharmaceutical compounds including inhibitors and receptor Antagonists. It can be used in the synthesis of polypeptides. | | Synthesis | To a mixed solution of (R)-azetidine-2-carboxylic acid (20 g, 200 mmol), water (200 mL) and dioxane (200 mL) was slowly added dropwise a solution of di-tert-butyl dicarbonate (Boc2O) in dioxane (100 mL) at 0 °C. After the dropwise addition was completed, the reaction mixture was stirred at room temperature for 1 hour. After the reaction was complete, the mixture was concentrated and ether (200 mL) and water (200 mL) were added to the residue. The aqueous layer was acidified to pH 3-4 with 2N hydrochloric acid and then extracted with ethyl acetate (200 mL). The organic layers were combined, dried over anhydrous sodium sulfate and concentrated to give (R)-N-BOC-azetidine-2-carboxylic acid (40 g) in quantitative yield.LRMS (M-100 + H*) m/z 102.1. | | References | [1] Patent: WO2008/16643, 2008, A2. Location in patent: Page/Page column 257
[2] Journal of Medicinal Chemistry, 1998, vol. 41, # 4, p. 407 - 412
[3] Patent: US6133253, 2000, A |
| | Boc-D-Azetidine-2-carboxylic acid Preparation Products And Raw materials |
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