- Method for preparing (S)-tetrahydro-1-naphthoic acid through high-efficiency resolution
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The invention relates to a preparation method of a palonosetron hydrochloride key intermediate (S)-1,2,3,4-tetrahydro-1-naphthoic acid as shown in a formula (I). The method comprises the following steps of adding a resolution agent for resolution by adopting 1,2,3,4-tetrahydro-naphthalene acid racemate as a raw material to obtain a salt (III) formed by a (S)-1,2,3,4-tetrahydro naphthalene acid and the resolution agent, and a salt (IV) formed by (R)-1,2,3,4-tetrahydro naphthalene acid and the resolution agent; carrying out salt removing on a compound III and a compound IV separately to obtain compounds (I) and (II); and carrying out racemization on the compound (II) under an alkaline condition to obtain a starting material 1,2,3,4-tetrahydro-naphthalene acid racemate and further carrying out resolution according to the steps. Therefore, the overall yield can be greatly improved, the production cost is reduced and environmental protection is facilitated. The preparation technology of the palonosetron hydrochloride key intermediate provided by the invention is different from the prior art, is safe, environmentally friendly, simple in operation and high in yield, and has relatively great practical value. The formula is as shown in the specification.
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Paragraph 0006; 0015; 0017
(2018/03/13)
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