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发明公开
CN110143886A 制备如妥洛特罗、氯丙那林、二氯异丙肾上腺素和索他洛尔的β-芳基氨基醇类药物的方法 有权

制备如妥洛特罗、氯丙那林、二氯异丙肾上腺素和索他洛尔的β-芳基氨基醇类药物的方法
摘要：
本发明提供了一种制备如妥洛特罗、氯丙那林、二氯异丙肾上腺素和索他洛尔的β-芳基氨基醇类药物的方法，所述β-芳基氨基醇类药物具有式4所示的化学结构，其中，所述方法包括以下步骤：(1)式1所示的芳基乙酮与卤化试剂和亚砜反应，得到式2所示的芳基酮醛和/或式3所示的1,1-二羟基芳基酮；(2)式2所示的芳基酮醛和/或式3所示的1,1-二羟基芳基酮与化学式为R1-NH2的胺类化合物进行亲核加成反应和还原剂存在下的还原胺化反应，得到β-芳基氨基醇类药物；
摘要（英）：

The invention provides a method for preparing beta-arylamino alcohol drugs such as tulobuterol, clorprenaline, dichloroisoprenaline and sotalol. The beta-arylamino alcohol drugs have a chemical structure represented by a formula 4 shown in the description. The method comprises the following steps: (1) reacting arylethanone represented by a formula 1 shown in the description with a halogenating agent and sulfoxide to obtain arylglyoxal represented by a formula 2 shown in the description and or 1,1-dihydroxyarylethanone represented by a formula 3 shown in the description; and (2) performing a nucleophilic addition reaction on the arylglyoxal represented by the formula 2 and/or the 1,1-dihydroxyarylethanone represented by the formula 3 and an amine compound having a chemical formula of R1-NH2, and performing a reductive amination reaction in the presence of a reducing agent to obtain the beta-arylamino alcohol drugs.

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