76 results about "Silyl enol ether" patented technology

The invention relates to a preparation method for oleanstada, which comprises: on catalyst action, using enolsiliconether and lauraldehyde to condense directly and obtain chiral hydroxyl hexadeketo ester; after eight steps contained protecting hydroxyl group, reducing and cyclization, obtaining the objective product with chemical formula as (I) for efficient fat-reducing. This method needs low cost.

The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 1713-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is —Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is —Si(R2)3.

The invention belongs to the field of drug synthesis and relates to an entecavir compound and a synthetic method of an intermediate of the entecavir compound. The novel synthetic method comprises: by taking (S)-3-hydroxyl dimethyl adipate as an initial raw material, preparing an intermediate 9 through hydroxyl TBS protection, Dieckmann condensation reaction, ketone protection to ketal, ester group reduction to hydroxyl, hydroxyl protection, deprotection, ketone to silyl enol ether and Rubottom oxidizing reaction; and preparing entecavir from the intermediate 9 through wittig reaction, Mitsunobu reaction, silicon preventing radical group removal and basic hydrolysis. The novel synthetic method provided by the invention is mild and easily controllable in reaction condition, simple to operate, high in product yield, high in purity and suitable for industrialized mass production.

The present invention discloses an AG-041R difluoro analog, a 3-difluoroalkyl substituted 3-amino quaternary carbon oxindole derivative and a synthesis method thereof, wherein the compound has a structure represented by the following formula, has potential biological activity and efficacy, provides powerful technical support for development of new drugs, and has high practical values. The synthesis process of the compound comprises: adding a catalyst to a reaction container, sequentially adding isatin imine, a solvent and a nucleophilic reagent difluoro silyl enol ether, stirring at a temperature of -78 DEG C -100 DEG C until the TLC display reaction is completed, and separating through column chromatography to obtain the product. According to the present invention, the synthesis method has characteristics of simple and easily-available raw materials, mild reaction condition, simple operation and wide substrate application range, and the compounds CF2-AG-041R and 3-difluoroalkyl substituted amino oxindole have potential and important medicinal values.

The invention belongs to the technical field of organic chemistry, and particularly relates to a synthesis method of an alpha, alpha-difluoro-beta-carbonyl sulfone compound. The method comprises the following steps: with acetonitrile as a solvent, carrying out a reaction on aryl diazonium salt, sodium metabisulfite and 2,2-difluoroenol silyl ether with Ru(bpy)3Cl2.6H2O being a photosensitizer under blue light irradiation to obtain the 2, 2-difluoroenol silyl ether photosensitizer, thereby generating aryl sulfonyl free radicals from aryl diazonium salt and sodium pyrosulfite under the action of blue light and a photosensitizer, performing addition reaction on 2,2-difluoroenol silyl ether to obtain a free radical intermediate, and performing single-electron oxidation on the free radical intermediate and an excited photosensitizer to obtain the alpha, alpha-difluoro-beta-carbonyl sulfone compound. The synthesis method of the compound has the advantages that with the aryl diazonium salt,sodium metabisulfite and 2,2-difluoroenol silyl ether, which are easy to obtain, being raw materials, strict reaction conditions such as strong base and ultralow temperature are not needed, so that the method has the advantages of strong functional group compatibility, wide substrate application range and the like, a series of alpha, alpha-difluoro-beta-carbonyl sulfone compounds can be efficiently synthesized, and the method has good academic guidance significance and industrial application value.

The invention provides a method for preparing an alpha-fluoro-beta-ethynyl ketone compound containing two chiral centers, belongs to the field of organic synthesis, and relates to a method for synthesizing an alpha-fluoro-beta-ethynyl ketone compound containing two chiral centers from fluorinated silyl enol ether and a propargyl compound by catalyzing an asymmetric propargyl substitution reaction, wherein the used chiral copper catalyst is generated from a copper salt and a chiral tridentate P,N,N-ligand in various polar and non-polar solvents in an in-situ manner. According to the present invention, with the method, the alpha-fluoro-beta-ethynyl ketone compounds containing two chiral centers and having various substituents can be conveniently synthzied, wherein the enantiomeric excess percentage is up to greater than 99%; and the method has characteristics of easily available raw materials, simple operation, mild reaction condition, high diastereoselectivity, high enantioselectivity, and the like.

The invention discloses a method for producing 6-ethylidene chenodeoxycholic acid by a continuous flow micro reactor. According to the method, pumping and conveying a solution of silyl enol ether intoa pipeline reactor through a pump; after cooling, mixing the solution with the cooled acetaldehyde solution in a mixer; then, continuously performing cooling in a pipeline reactor; next, mixing the materials with the cooled catalyst solution in another mixer; then, completing the reaction in the pipeline reactor. The operation is simple; the operation and the control of the production are easy; byproducts in the production process are few; the yield is high; the synchronous amplification is easy.

The invention discloses a preparation method of an alpha-alkenyl-alpha, alpha-difluoroaryl ketone compound and a product, and the preparation method comprises the following step: carrying out direct cross-coupling reaction on an aryl alkyne compound and difluoroenol silyl ether in a solvent under the action of a catalyst to obtain the alpha-alkenyl-alpha, alpha-difluoroaryl ketone compound. The difluoroenol silyl ether is used as a coupling substrate, so that the reaction has mild conditions and operation convenience, and the preparation method has the characteristics of simple post-treatment, cheap and small-amount catalyst, high economic benefit and the like.