- A NK - 1 receptor antagonists of the preparation method and its intermediate
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The invention relates to a preparation method of an NK-1 receptor antagonist and an intermediate thereof. The invention provides a preparation method of (5S, 8s)-8-{[1-(3, 5-bis-(trifluoromethyl)phenyl)-ethoxy]methyl}-8-phenyl-1, 7-diaza-spiro[4, 5]dec-2-one (formula I compound), which is prepared from a formula II compound, and also provides the formula II compound and a preparation method thereof. The method provided by the invention has the advantages of simple operation, mild reaction condition, high safety factor, little side reaction, high yield and high purity, lowers the production cost and operation risk, and is very suitable for large-scale industrial production. (formula II as shown in the specification).
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Paragraph 0100; 0102
(2018/07/30)
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- A practical entry to β-aryl-β-alkyl amino alcohols: Application to the synthesis of a potent BACE1 inhibitor
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The 1,2-addition of alkyl Grignard reagents to readily available N-tert-butanesulfinyl ketimines, bearing an α-silyloxy substituent, proceeds in high yields and excellent diastereocontrol. The utility of the present method was demonstrated by the synthesi
- Delgado, Oscar,Monteagudo, Antonio,Van Gool, Michiel,Trabanco, Andrés A.,Fustero, Santos
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scheme or table
p. 6758 - 6766
(2012/09/22)
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- Diastereoselective synthesis of (S)- and (R)-α-phenylserine by a sulfinimine-mediated strecker reaction
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A straightforward and efficient diastereoselective synthesis of (S)- and (R)-α-phenylserine is reported. The key step involves an asymmetric Strecker reaction of a chiral N-sulfinyl ketimine, which was obtained from the commercially available 2-hydroxyace
- Avenoza, Alberto,Busto, Jesus H.,Corzana, Francisco,Peregrina, Jesus M.,Sucunza, David,Zurbano, Maria M.
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p. 575 - 578
(2007/10/03)
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- Process for preparing optically active secondary alcohols having nitrogenous or oxygenic functional groups
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A process for preparing optically active secondary alcohols of the general formula (3), [wherein R1 is linear lower alkyl, an aromatic ring group, or the like; A is CH2NR2R3 or the like; n is an integer of 0 to 2; and * represents an asymmetric carbon atom] by asymmetrically hydrogenating a ketone compound of the general formula (1) having nitrogenous or oxygen functional group at any of the a-, β- and γ-positions, with selectivity among functional groups by the use of a ruthenium/optically active bidentate phosphine/diamine complex as the catalyst in the presence of hydrogen alone or together with a base. The optically active secondary alcohols obtained by the process are useful as drugs and intermediates for the preparation of drugs.
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- An alternative to the Swern oxidation
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A variety of alcohols have been oxidized under mild conditions by the DMSO-Ph3P·X2 complexes. The reaction does not produce any Pummerer product. A mechanism for the reaction is proposed.
- Bisai, Alakesh,Chandrasekhar,Singh, Vinod K.
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p. 8355 - 8357
(2007/10/03)
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- A Concise and Enantioselective Approach to Cyclobutanones by Tandem Asymmetric Epoxidation and Enantiospecific Ring Expansion of Cyclopropylidene Alcohols. An Enantiocontrolled Synthesis of (+)- and (-)-α-Cuparenones
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A tandem Katsuki-Sharpless asymmetric epoxidation and enantiospecific ring expansion of 2-alkyl(or 2-aryl)-2-cyclopropylideneethanols (1a-i) afforded chiral 1-alkyl(or 1-aryl)-1-(hydroxymethyl)cyclobutanones (3a-i) in high yields and high enantiomeric excess.These compounds are potentially valuable synthons for the enantioselective creation of the quaternary carbons.Hence, this enabled us to accomplish a concise and enantioselective total synthesis of both (+)- and (-)-cuparenones (11).
- Nemoto, Hideo,Ishibashi, Hiroki,Nagamochi, Masatoshi,Fukumoto, Keiichiro
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p. 1707 - 1712
(2007/10/02)
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