- Synthesis method of intermediate
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The invention provides a synthetic method of sofosbuvir intermediate (2E)-3-[(4S)-2,2-dimethyl-1,3-dioxolame-4-yl]-2-methyl-2-ethyl acrylate. The synthetic method adopts (R)-epoxy chloropropane as a raw material, and the sofosbuvir intermediate can be obtained by virtue of the acetonylidene protection and phosphorylation of triethyl phosphite, and the reaction with ethyl pyruvate. According to thesynthetic method, the (R)-epoxy chloropropane is used as the raw material and is low in price and easy to obtain; and other raw materials are conventional products in the market, so that the industrialized production cost is greatly decreased, the production cost of the intermediate can be reduced by 30 percent or more, the purity of a prepared target product is high, and the industrialized production prospect is great.
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Paragraph 0028; 0029
(2020/06/17)
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- A L - α - Ganong choline phosphate chemical synthesis method (by machine translation)
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The invention discloses a method for using the chlorinated choline salt, R - halogenated glycerin and ketone reagent as raw material preparation L - α - Ganong choline phosphate method, the resulting L - α - Ganong choline phosphate crude product by adsorption column, mixed bed and other purification processing of end high purity L - α - Ganong choline phosphate. By the invention chemical synthesis prepared by the method Ganong choline phosphate has high purity, simple steps of the reaction conditions, yield stability, while at the same time will not cause environmental pollution, having commercial production conditions. (by machine translation)
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Paragraph 0046
(2018/03/01)
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- Synthetic method of resolving agent hydrogen isopropylidene glycerol phthalate
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The invention relates to a resolving agent hydrogen isopropylidene glycerol phthalate. In the method, (S)-(-)-4-chloromethyl-2,2-dimethyl-1,3-dioxolane or (R)-(+)-4-chloromethyl-2,2-dimethyl-1,3-dioxolane is employed as a raw material and is reacted with hydrogen potassium phthalate to generate S/R-hydrogen isopropylidene glycerol phthalate. Compared with the prior art, the resolving agent is prepared directly from a commercial chiral raw material to directly synthesize the resolving agent hydrogen isopropylidene glycerol phthalate in a one-step manner. The raw materials are easy to obtain and are low in cost.
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Paragraph 0016; 0017
(2017/01/02)
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- Asymmetric synthesis of (4S,5S)-2-oxo-4-phenyloxazolidine-5-carboxylic acid using a 1,2-addition of PhMgBr to an N-sulfinimine derived from (R)-glyceraldehyde acetonide and (S)-t-BSA
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We report an asymmetric synthesis of (4S,5S)-2-oxo-4-phenyloxazolidine-5- carboxylic acid via stereoselective addition of phenylmagnesium bromide (PhMgBr) to an N-sulfinimine derived from (R)-glyceraldehyde acetonide. (S)- and (R)-Glyceraldehyde acetonides, important chiral synthons in synthetic organic chemistry, are prepared from the corresponding epichlorohydrin using an identical synthetic methodology.
- Babu, K. Chandra,Vysabhattar, Raman,Srinivas,Nigam, Satish,Madhusudhan,Mukkanti
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experimental part
p. 2619 - 2624
(2011/01/05)
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- Process for preparation of 1,3-dioxolane-4-methanol compounds
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PCT No. PCT/JP97/03165 Sec. 371 Date Feb. 8, 1999 Sec. 102(e) Date Feb. 8, 1999 PCT Filed Sep. 9, 1997 PCT Pub. No. WO98/11087 PCT Pub. Date Mar. 19, 1998A process for preparing easily and economically a 1,3-dioxolane-4-methanol compound in a racemic form or an optically active form with high purity and in high yield. The process comprises reacting an alkali metal or alkaline earth metal salt of an alcohol or a carboxylic acid with a halogenomethyl-1,3-dioxolane which is prepared by acetalizing a halogeno-1,2-propanediol of a formula (1) wherein X is a halogen atom, in an acid catalyst to conduct esterification or etherification, and then hydrolyzing the ester group and hydrogenolyzing the ether group to prepare a 1,3-dioxolane-4-methanol compound of a formula (5) wherein R1 and R2 are hydrogen atom, alkyl having 1 to 4 carbon atoms or phenyl, and R1 and R2 may form a cycloalkyl ring having 3 to 6 carbon atoms with the adjacent carbon atoms.
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- Method for preparing L-carnitine
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L-carnitine is prepared by a synthesizing process starting from D-mannitol. The synthesis is started with the formation of a D-mannitol ketonide (more specifically D-mannitol acetonide from D-mannitol and acetone, whereafter the D-mannitol is split by oxidation to give glyceraldehyde acetonide, which is further reduced to glycerol acetonide. Then the free hydroxyl group is exchanged with a halogen atom (chlorine) with the formation of chlorodihydroxy propane, the primary alcoholic group of which is functionalized with the acid chloride of a sulfonic acid (tosylchloride). The reaction of the tosyl derivative with the salt of hydrogen cyanide leads to the formation of the corresponding nitrile which, when reacted with trimethylamine gives carnitinonitrile. The nitrile group is now hydrolyzed to give L-carnitine chloride. The formation of L-carnitine can then be obtained by exchanging the chloride ion with a hydroxyl ion.
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