Author
Zhou Yi
Bio: Zhou Yi is an academic researcher. The author has contributed to research in topics: Wacker process & Lewis acid catalysis. The author has co-authored 3 publications.
Papers
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Patent•
04 Sep 2018
TL;DR: In this article, an anti-trypanosome anticancer natural product Cryptofolione synthesizing method was disclosed, which comprises the steps: after acrolein and silyl enol ether are utilized to perform Mukaiyama aldol reaction, sodium borohydride is used for reducing ketone into alcohol, and then pyridinium p-toluenesulfonate refluxes in a methylbenzene solution to obtain compound shown in a formula 5; after cinnamyl aldehyde and an evans
Abstract: The invention discloses an anti-trypanosome anticancer natural product Cryptofolione synthesizing method. The synthesizing method disclosed by the invention comprises the steps: after acrolein and silyl enol ether are utilized to perform Mukaiyama aldol reaction, sodium borohydride is used for reducing ketone into alcohol, and then pyridinium p-toluenesulfonate refluxes in a methylbenzene solutionto obtain compound shown in a formula 5; after cinnamyl aldehyde and an evans chiral aid are used for performing evans aldol reaction, diisobutyl aluminum hydride is used for reducing the cinnamyl aldehyde and the evans chiral aid at first, and then addition with metal indium activated 3-propylene bromine is performed to obtain compound shown in a formula 9; the compound shown in the formula 9 isresolved and purified for many times by kinetic resolution; the compound shown in the formula 9 and 2,2-diemthoxy propane can obtain fragment type 10 compound under the pyridinium p-toluenesulfonatecondition, the fragment type 10 compound and fragment type 5 compound can generate olefin metathesis reaction through a Grubbs secondary catalyst, and protecting groups of the fragment type 10 compound are removed under the hydrochloric acid condition to obtain Cryptofolione.
Patent•
04 Sep 2018
TL;DR: In this paper, a method for synthesizing weight loss drug orlistat key intermediate is presented, where n-dodecanal is utilized as a beginning raw material, orlist at intermediate compound (9) is prepared through multiple steps of reaction, and finally, or listat can be prepared through two steps of known reaction of chiral hydroxyl deprotection reaction andmistsunobu reaction.
Abstract: The invention discloses a method for synthesizing weight loss drug orlistat key intermediate. According to the method disclosed by the invention, n-dodecanal is utilized as a beginning raw material, orlistat intermediate compound (9) is prepared through multiple steps of reaction, and finally, orlistat can be prepared through two steps of known reaction of chiral hydroxyl deprotection reaction andmistsunobu reaction. A synthesizing strategy of the method disclosed by the invention is a typical linear strategy, a route design is simple and reasonable, an operation technology is convenient, reaction conditions are moderate, steps are few, a product yield is high, production cost is remarkably reduced, and the method is suitable for industrial preparation.
Patent•
22 Feb 2019
TL;DR: In this paper, a novel synthesis method of a natural product isomer (-)-6-epi-Porantheridine is presented, where a target molecule is synthesized by using a compound known in the formula 1 as a starting material through boc t-butoxycarbonyl protection and a series of reaction such as the asymmetric addition reaction of lewis acid catalysis, the Wacker oxidation reaction and ring-closing reaction.
Abstract: The invention discloses a novel synthesis method of a natural product isomer (-)-6-epi-Porantheridine. A target molecule is synthesized by using a compound known in the formula 1 as a starting material through boc t-butoxycarbonyl protection and a series of reaction such as the asymmetric addition reaction of lewis acid catalysis, the Wacker oxidation reaction and ring-closing reaction. The designof the whole route of the invention is unique and novel; the novel synthesis method is mild in reaction process and reaction conditions and fast in rate, has relatively little side reaction, and is simple and convenient in operation; conventional chemical reagents are utilized in the route; the raw materials are cheap and easily available; and the synthesis cost can be greatly reduced.