PATENT CLAIM ANALYSIS

Application Number: 15866899
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-05
Patent Classification: ["544", "331000"]

Abstract:
The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where R c  is an aryl sulfonic acid

Claim (Index 1):
A process for the preparation of a compound of formula VIII, the process comprising the steps of: (a) contacting 4-bromo-1-chloro-2-fluorobenzene with a metallating agent in an aprotic organic solvent to afford an organomagnesium compound, which is reacted with 2-chloro-N-methoxy-N-methylacetamide to afford 2-chloro-1-(4-chloro-3-fluorophenyl)ethanone (II); (b) contacting II with sodium formate and formic acid in aqueous ethanol to afford 1-(4-chloro-3-fluorophenyl)-2-hydroxyethanone (III) (c) contacting III with a ketoreductase to afford (R)-1-(4-chloro-3-fluorophenyl)ethane-1,2-diol (IV); (d) contacting IV with a silyl chloride (R a ) 3 SiCl and at least one base in a non-polar aprotic solvent to afford (V), and subsequently adding sulfonylchloride R b S(O) 2 Cl to afford VI, wherein R a  is independently in each occurrence C 1-6  alkyl or phenyl and R b  is selected from C 1-4  alkyl or phenyl, optionally substituted with 1 to 3 groups independently selected from C 1-3  alkyl, halogen, nitro, cyano, or C 1-3  alkoxy; (e) contacting 4-(2-(methylsulfonyl)pyrimidin-4-yl)pyridin-2(1H)-one (VII) with a strong base in an organic solvent and subsequently adding VI to afford XI; (f) treating XI with an oxidizing agent to afford I; (g) treating 1-methyl-1H-pyrazol-5-amine with a strong base in an aprotic solvent at reduced temperature and adding the compound of formula I to afford IX; and, (h) contacting IX with a de-silylating agent to afford VIII.

Metadata:
- Claim Count in Document: 32.0
- Percentile: 86.0
- Lexical Diversity: 1.16667
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14473311', '15183486', '15694124', '15345537', '12517874']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7423165320856866
- 35 USC 102 Novelty (BERT): 0.5248262882793462
- Combined Prediction Score: 0.7205675077050526
- Mean Citation Score: 316.3001220000001
- Max Citation Score: 318.93372
- Similarity Product: 205.21213004977227

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