| Use | 1-tert-butoxycarbonyl-1-methylhydrazine, also known as 1-boc-1-methylhydrazine, is a pharmaceutical raw material, the intermediate N,N,N'-trimethylhydrazine can be used for the preparation of alamolin. Anamolin, a ghrelin receptor agonist developed by Helsinn, Inc. (Helsinn), has been developed in patients with non-small cell lung cancer for the treatment of anorexia, treatment of cachexia constitution or unexpected weight loss. |
| preparation | 7.2g of methyl hydrazine sulfate (49.9mmol) was added to 144ml of water, cooled to 5 °c, and 4.6g of nahco3 solid was added, the pH was adjusted to 10 with aqueous NaOH solution, and 144ml of tetrahydrofuran solution of (Boc)2O(49.95mmol) was added dropwise thereto and stirred for 12H. The reaction was monitored by TLC to be complete (developing solvent: petroleum Ether/ethyl acetate = 2/1). Ethyl acetate extraction (100ml × 3), combined organic phase, saturated salt water washing, anhydrous sodium sulfate drying, reduced pressure concentration, 6.0g (yield: 82%) of 1-tert-butoxycarbonyl-1-methylhydrazine was obtained as a colorless transparent liquid. |
