159706-87-3

Usage

Uses

Used in Pharmaceutical Industry:
(S)-3-(4-Fluorophenyl)-4-benzyl-2-morpholinone is used as an anticonvulsant agent for its potential to treat seizure disorders. It has shown promising results in preclinical trials, indicating its effectiveness in managing convulsions and related symptoms.
(S)-3-(4-Fluorophenyl)-4-benzyl-2-morpholinone is also used as an analgesic agent, suggesting its potential to alleviate pain and discomfort in various conditions. Its ability to modulate pain signals makes it a candidate for the development of new pain management therapies.
Furthermore, (S)-3-(4-Fluorophenyl)-4-benzyl-2-morpholinone is used as a modulator of opioid receptors, indicating its potential applications in the treatment of pain and addiction. Its interaction with opioid receptors may offer new approaches to managing opioid dependence and withdrawal symptoms, as well as providing alternative pain relief options.
However, further research is needed to fully elucidate the pharmacological properties and potential therapeutic uses of (S)-3-(4-Fluorophenyl)-4-benzyl-2-morpholinone, ensuring its safety and efficacy in various medical applications.

InChI:InChI=1/C17H16FNO2/c18-15-8-6-14(7-9-15)16-17(20)21-11-10-19(16)12-13-4-2-1-3-5-13/h1-9,16H,10-12H2/t16-/m0/s1

Upstream product

• 5453-99-6 4-benzyl-morpholin-2-one 
• 352-34-1 4-fluoro-1-iodobenzene 
• 100-39-0 benzyl bromide 
• 1224387-68-1 (2-methoxy-2-oxo-(S)-1-phenylethyl) α-bromo(p-fluorophenyl)acetate 
• 104-63-2 N-Benzylethanolamine 
• 271583-38-1 2-(N-benzyl)amino-2-(4-fluorophenyl)acetamide 
• 200000-54-0 N-benzyl-4-fluorophenylglycine 
• 100-46-9 benzylamine 
• 459-57-4 4-fluorobenzaldehyde 
• 220130-49-4 [(diphenylmethyl)amino](4-fluorophenyl)acetonitrile 
• 187876-68-2 3-(S)-(4-Fluorophenyl)-4-benzyl-2-morpholinone 

Downstream Products

• 503537-21-1 (S)-2-Allyl-4-benzyl-3-(4-fluoro-phenyl)-morpholin-2-ol 
• 1296765-17-7 C₁₇H₁₈FNO₂ 
• 170729-77-8 (2R,3S)-4-benzyl-2-({1-[3,5-bis(trifluoromethyl)phenyl]-vinyl}oxy)-3-(4-fluorophenyl)morpholine 
• 472968-65-3 C₂₁H₂₉FN₃O₃P 
• 472968-64-2 Carbonic acid (2S,3S)-4-benzyl-3-(4-fluoro-phenyl)-morpholin-2-yl ester isopropyl ester 
• 472968-63-1 Dimethyl-carbamic acid (2S,3S)-4-benzyl-3-(4-fluoro-phenyl)-morpholin-2-yl ester 
• 1027926-21-1 Methanesulfonic acid (2S,3S)-4-benzyl-3-(4-fluoro-phenyl)-morpholin-2-yl ester 
• 195605-26-6 (5S,10S)-9-Benzyl-10-(4-fluoro-phenyl)-3-[2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-phenyl]-1,6-dioxa-9-aza-spiro[4.5]dec-3-ene 
• 195605-08-4 (3S,5S,10S)-10-(4-Fluoro-phenyl)-3-[2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-phenyl]-1,6-dioxa-9-aza-spiro[4.5]decane 

Relevant academic research and scientific papers

Chiral synthesis method of aprepitant intermediate and intermediate thereof (by machine translation)

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

Direct Synthesis of N-Alkyl Arylglycines by Organocatalytic Asymmetric Transfer Hydrogenation of N-Alkyl Aryl Imino Esters

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.

Dynamic kinetic resolution of (S)-mandelate-derived a-bromo esters in nucleophilic substitution and asymmetric syntheses of 3-substituted morpholin-2-ones

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.

AN IMPROVED PROCESS FOR THE PREPARATION OF APREPITANT

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.

PROCESS FOR PREPARATION OF APREPITANT

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.

An asymmetric synthesis of 3-aryl-1,4-oxazin-2-ones: Synthesis of a key intermediate of an NK1 receptor antagonist

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

Polymorphic form of a tachykinin receptor antagonist

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.

MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS

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.

Morpholinyl tachykinin receptor antagonists

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

MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS

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.