| 摘要 |
<p>PURPOSE: A method for preparing sitagliptin is provided to easily obtain sitagliptin with an eco-friendly method without expensive heavy metals such as Rh and Ru. CONSTITUTION: A method for preparing a compound of chemical formula 1 comprises a step of reacting a compound of chemical formula 10 with an amine protection group removing substance under the presence of carbonyl reducing substance. The method for preparing the compound of chemical formula 10 comprises: a step of introducing an amine protection group to L-aspartic acid to prepare a compound of chemical formula 4; a step of converting the compound of chemical formula 4 into anhydride to prepare a compound of chemical formula 5; a step of reacting the compound of chemical formula 5 with alcohol to prepare a compound of chemical formula 6; a step of reacting a compound of chemical formula 3 with the compound of chemical formula 6 to prepare a compound of chemical formula 7; a step of hydrolyzing the compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of reacting the compound of chemical formula 8 with a compound of chemical formula 16 to prepare a compound of chemical formula 9; and a step of reacting the compound of chemical formula 9 with a compound of chemical formula 17 to prepare a compound of chemical formula 10.</p> |
