5-[(2R)-2-Aminopropyl]-1-[3-(benzoyloxy)propyl]-2,3-dihydro-1H-indole-7-carbonitrile (2R,3R)-2,3-dihydroxybutanedioate synthesis
- Product Name:5-[(2R)-2-Aminopropyl]-1-[3-(benzoyloxy)propyl]-2,3-dihydro-1H-indole-7-carbonitrile (2R,3R)-2,3-dihydroxybutanedioate
- CAS Number:239463-85-5
- Molecular formula:C26H31N3O8
- Molecular Weight:513.55
239463-72-0
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239463-85-5
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Yield:239463-85-5 84.5%
Reaction Conditions:
with lithium hydroxide monohydrate;(2E)-but-2-enedioic acid in methanol at 15 - 20; for 8 h;Large scale;
Steps:
7 synthesis of 5-[2(R)-aminopropyl]-1-[3-(benzoyloxy)propyl]-7 cyano-indoline tartrate
In the 50L reactor, add 0.62Kg of fumaric acid and 6L of methanol,After stirring evenly, the temperature was raised to 50° C. to dissolve the solution, and then 1.5Kg of compound 10 and 10L of 98% methanol solution (water 2%) were added dropwise, and the system became turbid. Subsequently, the reaction solution was heated and refluxed (70-75°C) for 5 hours to obtain a yellow liquid, which was slowly cooled to 15-20°C, stirred at this temperature for 3 hours, filtered, and the filter cake was rinsed with cold methanol and dried. Dry to obtain 1.79Kg of 5-[2(R)-aminopropyl]-1-[3-(benzoyloxy)propyl]-7cyano-indoline tartrate. Yield 84.5%.
References:
CN114751852,2022,A Location in patent:Paragraph 0048-0050
496-15-1
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239463-85-5
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350797-56-7
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239463-85-5
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