PATENT CLAIM ANALYSIS

Application Number: 16243091
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2020-02
Patent Classification: ["null", "null"]

Abstract:
A method for preparing 5-(4-bromophenyl)-4,6-dichloropyrimidine is provided. The method comprises the steps of: preparing methyl p-bromophenylacetate (Intermediate I) by catalytic esterification of p-bromophenylacetic acid, and then reacting with dimethyl carbonate to synthesize 2-(4-bromophenyl)-malonic acid-1,3-dimethyl ester (Intermediate 2), cyclizing with formamidine hydrochloride to obtain 5-(4-bromophenyl)-4,6-dihydroxypyrimidine (Intermediate 3), and then chlorinating to give the product 5-(4-bromophenyl)-4,6-dichloropyrimidine. In the process of preparing Intermediate 1 in the present invention, a solid acid is used as a catalyst. Moreover, in the process of preparing Intermediate 2, sodium methoxide is used as a base in place of sodium hydride or sodium amide used in the prior art. Furthermore, Intermediate 3 is prepared by a one-pot process.

Claim (Index 1):
A method for preparing 5-(4-bromophenyl)-4,6-dichloropyrimidine, comprising:\n Step 1: adding p-bromophenylacetic acid and a solid acid catalyst to a reactor, then adding methanol, heating with stirring, and refluxing to react for 5-6 hours under reflux; and cooling the reaction solution to 30\u00b0 C. or below, filtering to recover the solid acid catalyst, distilling the resulting filtrate under reduced pressure to remove methanol, adding a hydrophobic solvent to dissolve the residue by stirring, washing the hydrophobic solvent with water, and concentrating under reduced pressure to obtain Intermediate 1 having a chemical structure (I) below; Step 2: adding sodium methoxide and methanol to Intermediate 1 obtained in Step 1, mechanically stirring, then adding dimethyl carbonate, replacing the air in the reactor with nitrogen, heating to 70-80\u00b0 C., and reacting for 4-8 hours, to obtain a mixture containing Intermediate 2 having a chemical structure (II) below; Step 3: adding formamidine hydrochloride to the mixture containing Intermediate 2 obtained in Step 2, heating to 20-30\u00b0 C. with stirring, and reacting for 15-17 hours, followed by post-treatment, to obtain Intermediate 3 having a chemical structure (III) below; and Step 4: chlorinating Intermediate 3 obtained in Step 3 to obtain the product 5-(4-bromophenyl)-4,6-dichloropyrimidine.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 99.0
- Lexical Diversity: 1.95946
- Patent Class: nan
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13521780', '15535413', '15521021', '14399929', '14673427']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.5293335418977647
- 35 USC 102 Novelty (BERT): 0.4878359974075053
- Combined Prediction Score: 0.5251837874487388
- Mean Citation Score: 222.156194
- Max Citation Score: 235.4971
- Similarity Product: 180.6436296911896

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