98977-36-7Relevant articles and documents
Multi-chiral nitrogen-substituted piperidinol derivative and preparation method thereof
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Paragraph 0017; 0019, (2021/10/11)
The invention belongs to the technical field of preparation of chiral piperidine alcohol compounds. The invention particularly relates to a multi-chiral nitrogen-substituted piperidinol derivative and a preparation method thereof. The 3 -hydroxypyridine serves as a starting raw material, and the corresponding substrate is obtained through catalytic hydrogenation reduction, amino protection, hydroxyl oxidation and Stork enamine - carbon alkylation to obtain the corresponding substrate. The process is simple, the reaction conditions are mild, and in particular, the ketone reducing liquid enzyme (KRED - 101) is selectively catalyzed, so that a chiral target product is obtained, and the yield is stable and the three wastes are few. The obtained piperidine heterocyclic derivative with the chiral center body has a plurality of drug activities and is suitable for industrial production.
A pharmaceutical intermediate N - BOC - 3 - piperidone preparation method (by machine translation)
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Paragraph 0055; 0059-0061; 0076-0077, (2018/03/01)
The invention belongs to the field of organic synthetic technology, in particular to a pharmaceutical intermediate N - BOC - 3 - piperidone of the preparation method. To solve the problems of the prior N - BOC - 3 - piperidone in the preparation method of catalyst used is 2, 2, 6, 6 - tetramethyl piperidine nitrogen oxygen free radical or its derivatives catalytic abilities and the catalytic activity is low, the problem of catalyst is difficult to be recycled. The preparation method comprises: the 3 - hydroxy piperidine and sodium carbonate, di-T-n-butyl is the reaction in a solvent, to prepare the N - BOC - 3 - hydroxy piperidine; the N - BOC - 3 - hydroxy piperidine and potassium bromide, catalyst, sodium hypochlorite in weakly alkaline conditions arranged below the reaction in a solvent, to obtain N - BOC - 3 - piperidone. Preparation method of this invention the use of cross-linked polystyrene [...] in 9 - aza bicyclo [3, 3, 1] - nonyl - 9 - oxygen free radical as the catalyst, the use of sodium hypochlorite solution to carry out oxidation, in the method, the catalyst is easily recycled, can improve the preparation with the yield of the product, reducing N - BOC - 3 - piperidone the production cost of the, and can reduce the pollution of the environment. (by machine translation)
A N - Boc - 3 - piperidone preparation method (by machine translation)
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Paragraph 0043; 0047; 0051; 0055; 0059; 0063, (2018/03/26)
The invention discloses a N - Boc - 3 - piperidone preparation method, which belongs to the technical field of organic synthesis. N - benzyl - 3 - hydroxy pyridine quaternary ammonium salt in the presence of a Lewis acid with potassium borohydride reduction reaction to obtain N - benzyl - 3 - piperidone; then after catalytic hydrogenation conditions with palladium of di-T-n-butyl reaction to obtain N - Boc - 3 - piperidone. Compared with the prior synthetic method, the invention one-step reaction will be N - benzyl - 3 - hydroxy pyridine quaternary ammonium salt selective reduction to obtain N - benzyl - 3 - piperidone, the reaction is fast, convenient separation of products, less side reaction, the advantages of synthetic route is simple. (by machine translation)