PATENT CLAIM ANALYSIS

Application Number: 15995098
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-09
Patent Classification: ["546", "208000"]

Abstract:
The present invention discloses a preparation method of cobimetinib (XL518, GDC-0973) (I). The preparation steps include: taking (2S)-2-piperidinecarboxylic acid as the raw material, performing acyl cyanation, hydrolysis, esterification and Boc protection to obtain an intermediate [2-oxo-2-((2S)-1-tert-butoxycarbonylpiperidin-2-yl)]acetate, performing an addition reaction, a reduction reaction and a cyclization reaction on the intermediate to obtain an intermediate (2S)-1-tert-butoxycarbonyl-2-(3-hydroxyazetidin-3-yl)piperidine, and performing a condensation reaction with a side chain to obtain the cobimetinib (I). The preparation method has the advantages of accessible raw materials, simple technique, high economy and environment friendliness, and is suitable for industrial production.

Claim (Index 2):
The preparation method of cobimetinib according to  claim 1 , wherein the cyanation reagent in the acyl cyanation reaction is sodium cyanide, zinc cyanide, cuprous cyanide or trimethylsilyl cyanide; the phase-transfer catalyst used in the acyl cyanation reaction is benzyl triethylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium chloride, tetrabutylammonium hydrogen sulfate, trioctyl methyl chloride ammonium, dodecyltrimethylammonium chloride or tetradecyltrimethylammonium chloride; the temperature of the acyl cyanation reaction is 50-150\u00b0 C.; and the reaction solvent is benzene/water, toluene/water, xylene/water or 1,2-dichloroethane/water in a volume ratio of 1-5/1.

Metadata:
- Claim Count in Document: 20.0
- Percentile: 93.0
- Lexical Diversity: 1.84507
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15952202', '14975785', '15206553', '16345744', '15575171']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7651885834104728
- 35 USC 102 Novelty (BERT): 0.5125757836648043
- Combined Prediction Score: 0.739927303435906
- Mean Citation Score: 259.266924
- Max Citation Score: 292.34512
- Similarity Product: 233.8388445634365

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

Dataset: test