PATENT CLAIM ANALYSIS

Application Number: 15575778
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2018-10
Patent Classification: ["544", "293000"]

Abstract:
The present invention relates to an improved process for the preparation of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethyl amino)-(2E)-2-butenamide (2Z)-2-butenedioate (1:2) represented by the following structural formula:

Claim (Index 1):
A process for the preparation of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-(2E)-2-butenamide (2Z)-2-butenedioate (1:2) compound of formula-1, comprising of;\n a) Treating 7-flouro-6-nitroquinazolin-4(3H)-one compound of formula-2 with a suitable chlorinating agent in presence of a suitable base in a suitable solvent to provide 4-chloro-7-fluoro-6-nitroquinazoline compound of formula-3, b) reacting compound of formula-3 in-situ with 3-chloro-4-fluoroaniline compound of formula-4 in presence of a suitable base in a suitable solvent to provide N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine compound of formula-5, which is optionally purifying from a suitable solvent to provide pure N-(3-chloro-4-fluoro phenyl)-7-fluoro-6-nitroquinazolin-4-amine compound of formula-5, c) reacting compound of formula-5 with (S)-tetrahydrofuran-3-ol compound of formula-6 in presence of a suitable base in a suitable solvent to provide (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-4-amine compound of formula-7, d) treating compound of formula-7 with a suitable reducing agent in a suitable solvent or mixture of solvents, optionally isolating 4-[(3-Chloro-4-fluorophenyl)amino]-6-amino-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline compound of formula-8, further treating the obtained compound with isopropanolic-HCl provides 4-[(3-Chloro-4-fluorophenyl)amino]-6-amino-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline dihydrochloride compound of formula-8a, e) optionally, purifying the obtained compound of formula-8a with a suitable solvent or mixture of solvents to provide pure compound of formula-8a, f) converting (E)-4-(dimethylamino)but-2-enoic acid compound of formula-9 or its salts into its acid chloride by using a suitable chlorinating agent in a suitable solvent, g) reacting the compound of formula-8a obtained from step (d) or step-(e) with the acid chloride compound of formula-9 obtained in step-(f) in presence of a suitable base in a suitable solvent to provide N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-(2E)-2-butenamide compound of formula-10, which is optionally purifying from a suitable solvent or mixture of solvents to provide pure N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-(2E)-2-butenamide compound of formula-10, h) treating compound of formula-10 with maleic acid in a suitable solvent to provide N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolin yl]-4-(dimethylamino)-(2E)-2-butenamide (2Z)-2-butenedioate (1:2) compound of formula-1.

Metadata:
- Claim Count in Document: 59.0
- Percentile: 97.0
- Lexical Diversity: 1.46154
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15516382', '15565996', '15553843', '13138429', '11997719']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.5261042132100088
- 35 USC 102 Novelty (BERT): 0.5246421316828849
- Combined Prediction Score: 0.5259580050572964
- Mean Citation Score: 289.474582
- Max Citation Score: 317.6971
- Similarity Product: 234.52780821849103

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