- Chiral synthesis method of aprepitant intermediate and intermediate thereof (by machine translation)
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The invention discloses a chiral synthesis method of aprepitant intermediate and a synthesis method of the, aprepitant intermediate, wherein the (2) synthesis method (3) comprises the following, shown in the following reaction formula: (1) the compound; I
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Paragraph 0042-0055
(2020/01/03)
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- Direct Synthesis of N-Alkyl Arylglycines by Organocatalytic Asymmetric Transfer Hydrogenation of N-Alkyl Aryl Imino Esters
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The organocatalytic asymmetric transfer hydrogenation of N-alkyl aryl imino esters for the direct synthesis of N-alkylated arylglycinate esters is reported. High yields and enantiomeric ratios were obtained, and tolerance to a diverse set of functional groups facilitated the preparation of more complex molecules as well as intermediates for active pharmaceuticals. A simple recycling protocol was developed for the Br?nsted acid catalyst which could be reused through five cycles with no loss of activity or selectivity.
- Mazuela, Javier,Antonsson, Thomas,Johansson, Magnus J.,Knerr, Laurent,Marsden, Stephen P.
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supporting information
p. 5541 - 5544
(2017/10/25)
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- Dynamic kinetic resolution of (S)-mandelate-derived a-bromo esters in nucleophilic substitution and asymmetric syntheses of 3-substituted morpholin-2-ones
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Dynamic kinetic resolution of (S)-mandelate-derived α-bromo esters in nucleophilic substitution reaction has been investigated. Substitutions with various alkyl amine nucleophiles in the presence of TBAI and DIEA can provide various α-amino esters up to 81% yield and 97:3 dr. Also, the substitution of α-bromo esters with N-substituted 2-aminoethanol nucleophiles and following spontaneous cyclization provides a practical protocol for asymmetric syntheses of 3-substituted morpholin-2-ones up to 95:5 er. ARKAT USA, Inc.
- Lee, Yoon Min,Kang, Kyoung Hee,Min, Hye-Min,Lim, Hyun Jin,Park, Eun-Hyung,Park, Yong Sun
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experimental part
p. 1 - 15
(2010/08/06)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF APREPITANT
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The present invention relates to an improved process for the preparation of Aprepitant of formula (I) and its intermediates. More particularly the present invention relates to the preparation of 3-(-S)-(4-fluorophenyl)-4-benzyl-2-morpholinone of Formula (III) or its salts thereof by reacting N-benzyl-(S)-(4-fluorophenyl) glycine of formula (II) with 1,2 dibromoethane in presence of an organic base.
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Page/Page column 7
(2009/03/07)
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- PROCESS FOR PREPARATION OF APREPITANT
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The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4- fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.
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Page/Page column 12-13
(2010/11/26)
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- An asymmetric synthesis of 3-aryl-1,4-oxazin-2-ones: Synthesis of a key intermediate of an NK1 receptor antagonist
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Pyrrolidine derived (S)-lactamide auxiliaries mediate a highly diastereoselective coupling reaction between racemic α-halo acids and N-benzylethanolamine. The adducts are readily cyclized upon treatment with a catalytic amount of TsOH giving the above tit
- Devine, Paul N.,Foster, Bruce S.,Grabowski, Edward J. J.,Reider, Paul J.
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p. 119 - 123
(2007/10/03)
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- Polymorphic form of a tachykinin receptor antagonist
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This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
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- MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS
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Substituted heterocycles of the general structural formula: STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
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- Morpholinyl tachykinin receptor antagonists
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This invention provides methods of treating a physiological disorder associated with an excess of tachykinins in a mammal which comprises administering to a mammal in need of said treatment a compound selected from a series of substituted morpholines. Thi
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- MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS
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Substituted heterocycles of the general structural formula: STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
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- PROCESS FOR PREPARING MORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS
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Substituted heterocycles of the general structural formula: STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
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- MORPHOLINE COMPOUNDS ARE PRODRUGS USEFUL AS TACHYKININ RECEPTOR ANTAGONISTS
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Substituted heterocycles of the general structural formula: STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, and emesis.
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- Synthesis of N-benzyl-3-(S)-(+)-(4-fluorophenyl)-1,4-oxazin-2-one via a crystallisation induced asymmetric transformation
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The simple and efficient preparation of enantiomerically pure N-benzyl-3-(S)-(+)-(4-fluorophenyl)-1,4-oxazin-2-one by a crystallisation induced asymmetric transformation of its racemate is reported. A key feature of this process is the use of [(1S)-(endo,
- Alabaster, Ramon J.,Gibson, Andrew W.,Johnson, Simon A.,Edwards, John S.,Cottrell, Ian F.
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p. 447 - 450
(2007/10/03)
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- TREATMENT OF EMESIS WITH MORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS
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Substituted heterocycles of the structural formula: STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, emesis and nausea.
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