98977-36-7Relevant articles and documents
Multi-chiral nitrogen-substituted piperidinol derivative and preparation method thereof
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, (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.
An investigation into the role of 2,6-lutidine as an additive for the RuCl3-NaIO4 mediated oxidative cleavage of olefins to ketones
Watson, David W.,Gill, Matthew,Kemmitt, Paul,Lamont, Scott G.,Popescu, Mihai V.,Simpson, Iain
supporting information, p. 4479 - 4482 (2018/11/23)
2,6-Lutidine has been identified as a beneficial additive for the oxidative cleavage of olefins to ketones by NaIO4 in the presence of catalytic RuCl3, improving the yield and shortening the reaction times. In the absence of 2,6-lutidine reactions stalled at the diol intermediate with incomplete conversion to the desired ketones. The reaction protocol described herein also avoids the use of harmful solvents such as CCl4 and DCE and is tolerant of a range of functional groups.
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)