Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Dichloromethane | HCID 6344 | — |
| Reactant | (Diethylamino)sulfur trifluoride | HCID 123472 | — |
| Reactant | Acetone cardice | HCID 18522661 | — |
| Reactant | HCID 25167673 | HCID 25167673 | — |
| Product | HCID 67119787 | HCID 67119787 | 34.8% |
Reaction Steps
N-(1-(4-methoxyphenyl)ethyl)-4-benzoylmethyl-4-piperidinol (III-19) is firstly prepared according to the method of synthesis and post-treatment in Example 19. 1.41 g (4.0 mmol) of N-(1-(4-methoxyphenyl)ethyl)-4-benzoylmethyl-4-piperidinol is taken and dissolved into 20 ml of anhydrous dichloromethane and cooled with dry ice-acetone with temperature controlled at below <−70° C. The reaction solution is added dropwise a dichloromethane solution (8 mol, 25 ml) of DAST under protection of nitrogen gas. After completion of addition, the temperature is maintained at −75° C. and reacting for 1 hour, and the temperature is raised slowly and maintained at −10° C. and reacting for 2 hours. Then operating according to the post-treatment method in General Method six obtains 0.57 g of a white crystal, with yield of 34.8%.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08501778B2 |
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| Source dataset | uspto-grants-2013_08 |
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| ORD ID | ord-791b3ceb356f4be3b0a85e04568f7b8f |
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| Source note | uspto-grants-2013_08 |
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