PATENT CLAIM ANALYSIS

Application Number: 16087308
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-04
Patent Classification: ["548", "430000"]

Abstract:
Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production.

Claim (Index 17):
The method of  claim 16 , wherein\n in step (a), the base is selected from the group consisting of sodium hydride, potassium tert-butoxide, sodium hydroxide, potassium hydroxide or cesium carbonate, preferably sodium hydroxide or potassium hydroxide; a molar ratio of the compound shown by Formula V to the base is 1:1 to 1:3, preferably 1:1.1 to 1:2; a molar ratio of the compound shown by Formula V to the compound shown by Formula VI is 1:1 to 1:3, preferably 1:1.1 to 1:1.5; a reaction solvent is selected from the group consisting of N,N-dimethylformamide, dimethyl sulfoxide or acetonitrile, preferably dimethyl sulfoxide, a reaction temperature is 25 to 75\u00b0 C., preferably 55 to 65\u00b0 C.; in step (b), when R 1  is tert-butoxycarbonyl, and when removing the protecting group of amino under an acidic condition, the acid is selected from the group consisting of sulfuric acid, trifluoroacetic acid, hydrofluoric acid or hydrochloric acid, preferably hydrochloric acid; a reaction solvent used is selected from the group consisting of methanol, ethanol, ethyl acetate or a mixed solvent thereof, preferably a mixed solvent of ethanol and ethyl acetate, more preferably a volume ratio of ethanol to ethyl acetate is 2:3; a reaction temperature is controlled to be 20 to 70\u00b0 C., preferably 50 to 60\u00b0 C.; in step (c), when Y in the compound shown by Formula IX is a halogen, preferably chlorine, bromine or iodine; and when Y is a sulfonyloxy, preferably a sulfonyloxy, p-toluenesulfonyloxy or methanesulfonyloxy; the base is selected from the group consisting of potassium carbonate, sodium carbonate, sodium hydroxide or potassium hydroxide, preferably potassium carbonate; a molar ratio of the compound shown by Formula VIII to the compound shown by Formula IX is 1:1 to 1:3, preferably 1:1.4 to 1:2; a molar ratio of the compound shown by Formula VIII to the base is 1:1.5 to 1:4, preferably 1:2 to 1:3.5; a reaction solvent used is selected from the group consisting of methanol, ethanol, acetonitrile, water or a mixed solvent thereof, preferably a mixed solvent of ethanol and water; in step (d), a reaction solvent used is selected from the group consisting of methanol, ethanol or isopropanol, preferably ethanol; a molar ratio of the compound shown by Formula XI to phosphoric acid is 1:0.95 to 1.05; a reaction temperature is controlled to be 20 to 80\u00b0 C., preferably 60 to 70\u00b0 C.

Metadata:
- Claim Count in Document: 7.0
- Percentile: 97.0
- Lexical Diversity: 1.47692
- Patent Class: 548.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15514326', '15763676', '16083485', '13994085', '16345744']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7523686481799554
- 35 USC 102 Novelty (BERT): 0.5150929434974502
- Combined Prediction Score: 0.7286410777117049
- Mean Citation Score: 262.935172
- Max Citation Score: 271.25452
- Similarity Product: 177.92376241626263

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