PATENT CLAIM ANALYSIS

Application Number: 16064003
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2019-01
Patent Classification: ["544", "333000"]

Abstract:
Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula 1, the product is prepared via compounds III and IV. The synthesis method adjusts the feeding means, and the reaction conditions are mild and controllable, thereby reducing the production of impurity A, avoiding the use of highly toxic metal lead, and eliminating the risk of highly toxic metal remaining in a drug. The product has a higher purity and significant industrial application value.

Claim (Index 1):
A method for synthesizing an important intermediate condensation compound of formula II of Voriconazole or an acid addition salt thereof, comprising reacting a compound of formula III with a compound of formula IV in an aprotic organic solvent at a certain reaction temperature, in the presence of zinc and a Lewis acid, with or without an activator, as shown in a reaction scheme 1, wherein the method comprises following steps:\n (a1) mixing the compound of formula III, zinc and the Lewis acid with the aprotic organic solvent to form a suspension; (b1) mixing the compound of formula IV with the aprotic organic solvent, optionally in the presence of the activator, to form a solution; (c1) adding slowly the solution formed in step (b1) into the suspension formed in step (a1) and reacting to provide the intermediate condensation compound of formula II; and (d1) optionally converting the intermediate condensation compound of formula II to an acid addition salt thereof; or, (a2) mixing the compound of formula III, zinc and the Lewis acid with the aprotic organic solvent to form a suspension; (b2) mixing the compound of formula IV with the aprotic organic solvent to form a solution; (c2) adding slowly the solution formed in step (b2) into the suspension formed in step (a2), optionally in the presence of the activator and reacting to provide the intermediate condensation compound of formula II; and (d2) optionally converting the intermediate condensation compound of formula II to an acid addition salt thereof; or, (a3) mixing the compound of formula III, the compound of formula IV, and the Lewis acid with the aprotic organic solvent to form a suspension; (b3) adding zinc into the suspension, optionally in the presence of the activator, to provide the intermediate condensation compound of formula II; and (c3) optionally converting the intermediate condensation compound of formula II to an acid addition salt thereof;

Metadata:
- Claim Count in Document: 41.0
- Percentile: 94.0
- Lexical Diversity: 1.53125
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['11120739', '12671418', '13257003', '15193385', '16073929']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7753624887222397
- 35 USC 102 Novelty (BERT): 0.4928591088662018
- Combined Prediction Score: 0.7471121507366358
- Mean Citation Score: 238.534274
- Max Citation Score: 241.54471
- Similarity Product: 174.83082500120517

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