- Synthesis method of atropine and atropine sulfate
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The invention provides a synthesis method of atropine and atropine sulfate, which comprises the following steps: carrying out acetylation reaction on tropine acid to form acetyl tropine acid, reactingthe acetyl tropine acid with a chlorination reagent to form acyl chloride, reacting the acyl chloride with tropine alcohol, removing acetyl to obtain atropine, and salifying atropine and sulfuric acid to obtain atropine sulfate. The whole synthesis process can be completed by adopting a one-pot reaction, additional steps for completing the process by isolating intermediates are avoided, the reaction conditions are mild, the steps are simple, the yield is high, the purity is high, and the method is suitable for large-scale industrial production.
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- Construction of 8-Azabicyclo[3.2.1]octanes via Sequential DDQ-Mediated Oxidative Mannich Reactions of N-Aryl Pyrrolidines
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A concise synthesis of 8-azabicyclo[3.2.1]octanes via sequential oxidative Mannich reactions is described. This approach involves an intermolecular oxidative Mannich coupling reaction between N-aryl pyrrolidines with TMS enol ether and a subsequent intramolecular oxidative Mannich cyclization of the corresponding silyl enol ether. DDQ is used as a key oxidant for both reactions.
- Jo, Hanbyeol,Hassan, Ahmed H. E.,Jung, Seung Young,Lee, Jae Kyun,Cho, Yong Seo,Min, Sun-Joon
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p. 1175 - 1178
(2018/02/23)
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- PROCESS FOR PREPARATION OF ATROPINE
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A process for the production of atropine is provided. The process provides for a new, efficient and commercially feasible synthetic process for the preparation of atropine and atropine salts. In one aspect, a one pot process for the synthesis of atropine is provided. The process provides excellent yield and can be used to prepare commercial 5 scale batches of atropine or atropine salts. The process avoids the additional steps of having to isolate intermediates to complete the process and has the advantage of proceeding efficiently at ambient temperature for many of the steps. The process includes providing acetyltropoyl chloride and reacting the acetyltropoyl chloride with tropine followed by a contact with an acid to form atropine.
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Page/Page column 8
(2016/03/12)
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- Total Synthesis of (±)-Scopolamine: Challenges of the Tropane Ring
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Scopolamine was synthesized using 6,7-dehydrotropine as a key intermediate. Rhodium-catalyzed [4 + 3] cycloaddition chemistry and a modified Robinson-Sch?pf reaction were each independently evaluated for their utility in constructing the tropane core. Both synthetic approaches gave comparable overall yields.
- Nocquet, Pierre-Antoine,Opatz, Till
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p. 1156 - 1164
(2016/03/05)
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