1185503-10-9

Upstream product

• 104-63-2 N-Benzylethanolamine 
• 1765-93-1 4-fluoroboronic acid 
• 1185503-03-0 4-benzyl-3-(4-fluorophenyl)morpholin-2-ol 
• 459-22-3 4-fluorophenylacetonitrile 
• 187876-68-2 3-(S)-(4-Fluorophenyl)-4-benzyl-2-morpholinone 

Downstream Products

• 1185503-13-2 C₁₉H₁₈Cl₃FN₂O₂ 
• 1185503-15-4 (+/-)-trans-4-benzyl-2-[2-(3,5-bis-trifluoromethylphenyl)ethoxy]-3-(4-fluorophenyl)morphine 
• 170729-80-3 aprepitant 
• 171338-27-5 [2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine 
• 380499-07-0 (2R)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-5,6-dihydro-2H-1,4-oxazine 
• 380499-06-9 (2R,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine 

Relevant academic research and scientific papers

Preparation method of important intermediate (2S, 3R)-4-benzyl-3-(4-fluorophenyl)morpholine-2-ol for aprepitant synthesis

The invention relates to a preparation method of an important intermediate (2S, 3R)-4-benzyl-3-(4-fluorophenyl)morpholine-2-ol for aprepitant synthesis. (2S, 3R)-4-benzyl-3-(4-fluorophenyl)morpholine-2-ol is prepared from 2-(4-fluorophenyl)acetonitrile as an initial raw material through cyclization, oxidation rearrangement, catalytic hydrogenation, benzyl protection, selective reduction and chiral resolution. The preparation method has simple processes, low equipment requirement, less process wastes, less environmental pollution and high product purity.

PREPARATION OF MORPHOLINE DERIVATIVES

This invention relates to processes and intermediates for the stereoselective morpholine derivatives. The invention in particular allows the stereoselective preparation of the drugs aprepitant and fosaprepitant.

PREPARATION OF APREPITANT

A process for preparing aprepitant.