28924-25-6Relevant articles and documents
Preparation method of terbutaline sulfate and B crystal form thereof
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Paragraph 0017; 0039; 0044-0047; 0054; 0058-0059, (2021/01/29)
The invention relates to a preparation method of terbutaline sulfate and a B crystal form thereof, which comprises the following steps: sequentially carrying out bromination, reduction reaction and substitution reaction to obtain 1-[3, 5-bis (benzyloxy) phenyl]-2-(tert-butylamino) ethanol; reacting 1-[3, 5-di (benzyloxy) phenyl]-2-(tert-butylamino) ethanol with a reducing agent and a catalyst, performing salifying with sulfuric acid to obtain a terbutaline sulfate crude product, and crystallizing the terbutaline sulfate crude product under a heating reflux condition to obtain the terbutaline sulfate medicinal B crystal form. Raw materials and auxiliary materials used in the method are cheap and easy to obtain, highly toxic and explosive reagents are avoided in the reaction process, the whole reaction route is short, operation is easy and convenient, reaction conditions are mild and safe, the yield of the obtained finished product terbutaline sulfate and the medicinal B crystal form thereof is high, the yield of terbutaline sulfate is 83% or above, and the yield of the medicinal B crystal form is 70% or above, and industrialized production can be achieved easily.
Method for synthesizing terbutaline
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Paragraph 0034; 0039-0040, (2020/02/10)
The invention discloses a method for synthesizing terbutaline. The method comprises the following steps: reacting a compound I with selenium dioxide to obtain a compound II; reacting the compound II with tert-butylamine to obtain a compound III; reacting the compound III with a reducing agent to obtain a compound IV; and reacting the compound IV with a catalyst to remove benzyloxy to obtain terbutaline. The synthesis method has the advantage that the generation of impurity alpha-bromo-3, 5-dibenzyloxyacetophenone is avoided.