1279032-31-3Relevant articles and documents
Method for preparing (1R, 3S)-3-aminocyclopentanol hydrochloride
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Paragraph 0030; 0046-0048; 0054-0058, (2021/03/31)
The invention discloses a method for preparing (1R, 3S) 3-aminocyclopentanol hydrochloride, belongs to the field of organic chemical synthesis, and provides a process route to overcome the defects ofhigh price, difficulty in chiral control and the like in the prior art. The process route comprises the following steps: 1) oxidizing tert-butyl carbonate hydroxylamine into tert-butyl carbonate nitrosyl under the catalysis of copper chloride and 2-ethyl-2-oxazoline, then carrying out a hetero Diels-Alder reaction with cyclopentadiene in situ; 2) selectively reducing nitrogen-oxygen bonds in a zinc powder-acetic acid reaction system; 3) under the catalysis of lipase, reacting with vinyl acetate to optically and selectively realize chiral resolution; 4) reducing double bonds through palladium carbon hydrogenation; 5) under the alkaline condition of lithium hydroxide-methanol, performing deacetylation protection; and 6) removing tert-butyl carbonate protection in a hydrogen chloride isopropanol acid solution prepared from acetyl chloride and isopropanol in situ, and forming hydrochloride in situ to obtain a target product. The synthetic method has the beneficial effects that the synthetic method has the characteristics of novel and short route, high optical purity, low cost and the like.
Preparation method of (1R, 3S)-3-amino-1-cyclopentanol hydrochloride
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Paragraph 0024, (2019/12/29)
The invention provides a preparation method of (1R, 3S)-3-amino-1-cyclopentanol hydrochloride. A target compound is synthesized through a chiral induction method, and specifically, cheap chiral hydroxy acid is used as a raw material and reacted with hydro
Intermediate for preparing bictegravir and preparation method thereof
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, (2019/01/08)
The invention relates to the technical field of a drug, and concretely relates to an intermediate for preparing bictegravir and a preparation method thereof. The present invention provides two novel types of compounds and three routes for preparation of a compound (VI). Through substrate induction, chiral catalysis or synergistic effect of substrate induction and chiral catalysis, the stereoselectivity of a Diels-Alder reaction can be greatly improved, and a high chiral purity of a common intermediate (III) can be obtained; cut-out of N-O bond and reduction the double bond use catalytic hydrogenation, which can be environmentally friendly; the reaction conditions are mild, the yield is higher than the existing preparation method, the method is economic and effective, and is adapted to large-scale industrial production.