- Preparation method of important intermediate (2S, 3R)-4-benzyl-3-(4-fluorophenyl)morpholine-2-ol for aprepitant synthesis
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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.
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- PREPARATION OF MORPHOLINE DERIVATIVES
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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.
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Page/Page column 11-12; 4
(2009/10/21)
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