(2S,3R)-1-substituted benzyl-2-allyl-3-hydroxypiperidine and preparation method thereof
A technology of hydroxypiperidine and allyl, which is applied in the field of 3-hydroxypiperidine derivatives and their preparation, can solve the problem that the synthesis method is not reported in literature and the like, achieves good market application prospects, high yield, and easy availability of raw materials Effect
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[0023] The preparation method of the present embodiment comprises the following steps:
[0024] 1. (S)-1-(N-benzylpyrrol-2-yl)-3-buten-1-ol (compound 5 ) preparation
[0025]
[0026] Add 48.6 g Mg chips (2.025 mol) to a 1000 mL four-neck flask, N 2 Stir vigorously overnight under protection to make it fully activated; add iodine in a catalytic amount (iodine as a catalyst), vacuumize, N 2 Add 400 mL of dry diethyl ether under protection (the whole process is reacted under strict anhydrous and oxygen-free conditions); put 30 mL of allyl bromide (0.35 mol) in a constant pressure dropping funnel, add about 20 drops, and stir Let it initiate the reaction (the color of iodine fades); then transfer to an ice bath, control the temperature at 0-5 °C, dilute allyl bromide with 60 mL of dry ether, and slowly add it dropwise to the system. About 17 h; after the dropwise addition, continue to react for 1 h; to obtain allyl magnesium bromide, the obtained allyl magnesium bromide is ...
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