PATENT CLAIM ANALYSIS

Application Number: 16076486
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-02
Patent Classification: ["564", "155000"]

Abstract:
The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

Claim (Index 1):
A process for the preparation of Lacosamide compound of the formula (I) comprising:\n i) N-Boc protection of D-serine at 50\u00b0 C. for the duration of 1-2 hoursusing Boc-anhydride in presence of sodium hydroxide as a base and water as a solvent to obtain N-Boc-D-serine, ii) Coupling of carboxylic acid moiety of N-Boc-D-serine produced in step i), with benzyl amine in presence of ethyl chloroformate and N-methyl morpholine at 10 to 15\u00b0 C. to obtain tert-butyl [(2R)-1-(benzyl amino)-3-hydroxy-1-oxopropan-2-yl]carbamate, iii) O-methylation of tert-butyl [(2R)-1-(benzyl amino)-3-hydroxy-1-oxopropan-2-yl]carbamate produced in step ii), with dimethyl sulfate in presence of potassium hydroxide as a base and dichloromethane as a solvent in the absence of PTC to generate tert-butyl [(2R)-1-(benzylamino)-3-methoxy-1-oxopropan-2-yl]carbamate, iv) Hydrolysis of N-Boc of tert-butyl [(2R)-1-(benzylamino)-3-methoxy-1-oxopropan-2-yl]carbamate produced in step iii) withalcoholic HCl at 50\u00b0 C. to produce hydrochloride salt of [(2R)-1-(benzylamino)-3-methoxy-1-oxopropan-2-yl]carbamate and subsequently N-acetylation of hydrochloride salt of (2R)-1-(benzylamino)-3-methoxypropanamide in presence of Sodium acetate without isolating free base (2R)-1-(benzylamino)-3-methoxypropanamide, to produce Lacosamide having chemical name (2R)-2-(acetylamino)-N-benzyl-3-methoxy propanamide.

Metadata:
- Claim Count in Document: 7.0
- Percentile: 96.0
- Lexical Diversity: 1.26316
- Patent Class: 564.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['13811707', '13577804', '13577367', '13274718', '13574833']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6783654307513677
- 35 USC 102 Novelty (BERT): 0.534054775056741
- Combined Prediction Score: 0.6639343651819051
- Mean Citation Score: 255.557662
- Max Citation Score: 294.76846
- Similarity Product: 236.3128863745356

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 0
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test