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ENHANCED PREPARATION METHOD OF DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATES THEREOF

机译:二肽肽酶-IV抑制剂的增强制备方法及其中间体

摘要

PURPOSE: A producing method of a dipeptidyl peptidase-iv inhibitor and its intermediate is provided to reduce the manufacturing cost for the dipeptidyl peptidase-iv inhibitor and the intermediate. CONSTITUTION: A producing method of a dipeptidyl peptidase-iv inhibitor intermediate marked with chemical formula 2 comprises the following steps: ring opening an epoxide ring of a compound marked with chemical formula 5 from a reaction formula 1 using a grinard reactant, to form a compound marked with chemical formula 6; reacting the compound marked with the chemical formula 6 with sodium azide to form a compound marked with chemical formula chemical formula 7; reacting the compound marked with the chemical formula 7 with triphenylphosphine to form a compound marked with chemical formula 8; and ring opening the outcome to form a compound marked with chemical formula 9 before hydrolyzing the compound.
机译:目的:提供一种二肽基肽酶-iv抑制剂及其中间体的生产方法,以降低二肽基肽酶-iv抑制剂及其中间体的生产成本。组成:化学式2标记的二肽基肽酶-iv抑制剂中间体的生产方法包括以下步骤:使用格林纳德反应物从反应式1中将化学式5标记的化合物的环氧环开环以形成化合物用化学式6标记;使化学式6所示的化合物与叠氮化钠反应形成化学式7所示的化合物。使化学式7所示的化合物与三苯基膦反应,形成化学式8所示的化合物。在水解该化合物之前,将结果开环以形成化学式9所示的化合物。

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