170729-77-8

Upstream product

• 785-56-8 3,5-bis(trifluoromethyl)phenyl carboxylic acid chloride 
• 219821-32-6 N-benzyl-3-(R)-(p-fluorophenyl)morpholin-2-one 
• 159706-87-3 4-benzyl-3-(4-fluorophenyl)morpholin-2-one 
• 219821-44-0 C₂₆H₂₀F₇NO₃*ClH 
• 1296765-17-7 C₁₇H₁₈FNO₂ 

Downstream Products

• 219821-44-0 C₂₆H₂₀F₇NO₃*ClH 
• 1215294-43-1 C₂₆⁽¹⁴⁾CH₂₂F₇NO₂ 

Relevant academic research and scientific papers

AN IMPROVED PROCESS FOR THE PREPARATION OF APREPITANT

The present invention relates to an improved process for the preparation of aprepitant compound of formula- (I) as well as novel polymorphs of its intermediates.

PROCESS FOR PURIFICATION OF APREPITANT

The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2

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 PURIFICATION OF APREPITANT

The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[I (RS)- [3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl- methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having mean particle size of less than about 11.5 microns, process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having the content of diastereomeric impurity of 1.1 % is dissolved in ethyl acetate at 700C, the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0 - 50C to give pure aprepitant substantially free of diastereomeric impurity.

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.

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.

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.

PROCESS FOR PREPARING MORPHOLINE 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.

MORPHOLINE COMPOUNDS ARE PRODRUGS USEFUL AS 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.