PATENT CLAIM ANALYSIS

Application Number: 15779910
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-12
Patent Classification: ["544", "132000"]

Abstract:
The present invention relates to a novel process for the preparation of intermediate of fosaprepitant dimeglumine. The present invention particularly relates to a process for the preparation of fosaprepitant dibenzyl ester, an intermediate of fosaprepitant dimeglumine, which is simple, easy to handle on commercial scale and efficient.

Claim (Index 4):
A process for the in-situ preparation of 1-deoxy-1-(methylamino)-D-Glucitol[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl) phenyl] ethoxyl-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl] phosphonate (2:1) salt (fosaprepitant dimeglumine) of formula I, comprising the steps of, (i) treating aprepitant of formula III with tetrabenzyl pyrophosphate using a base in the presence of a solvent at a temperature of \u221235\u00b0 C. to 0\u00b0 C. for 1 h to 4 h to obtain fosaprepitant dibenzyl ester, (ii) adding at least one solvent or a mixture of solvents to the reaction mass obtained in step (i), (iii) adding an inorganic acid to the reaction mass obtained in step (ii), (iv) concentrating the reaction mass obtained in step (iii), (v) adding at least one solvent or a mixture of solvents thereof to the reaction mass obtained in step (iv), (vi) filtering the reaction mass obtained in step (v) to obtain a residue, Residue-A, (vii) adding at least one solvent or a mixture of solvents thereof to the residue obtained in step (vi), (viii) filtering the reaction mass obtained in step (vii) to obtain a residue, Residue-B, (ix) adding at least one solvent or a mixture of solvents thereof to the residue obtained, in step (viii), (x) filtering the reaction mass obtained in step (ix) and concentrating the filtrate to yield fosaprepitant dibenzyl ester of purity >96% as an oil, (xi) dissolving the oil obtained in step (x) in at least one solvent or a mixture of solvents thereof, (xii) adding N-methyl-D-glucamine and Pd/C to the reaction mass obtained in step (xi) and hydrogenating the reaction mass for 8 h to 14 h at 2 kg to 8 kg pressure, (xiii) filtering the reaction mass obtained in step (xii), (xiv) adding metal scavenger to the reaction mass obtained in step (xiii) and stirring for 8 h to 14 h, (xv) obtaining fosaprepitant dimeglumine of purity >99% from the resulting reaction mass of step (xiv) on further work-up.

Metadata:
- Claim Count in Document: 8.0
- Percentile: 93.0
- Lexical Diversity: 1.67742
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14123290', '13003885', '15728972', '15165643', '14773397']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7374205020956718
- 35 USC 102 Novelty (BERT): 0.5209652733884619
- Combined Prediction Score: 0.7157749792249508
- Mean Citation Score: 275.33036400000003
- Max Citation Score: 328.53616
- Similarity Product: 277.25404305757525

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test