PATENT CLAIM ANALYSIS

Application Number: 15756214
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-11
Patent Classification: ["540", "222000"]

Abstract:
The present invention relates to a highly convergent method for the synthesis and purification of ceftolozane and intermediates starting from 7-aminocephaiosporanic acid (7-ACA).

Claim (Index 1):
A method for preparing a compound of formula wherein R 6\u2032  is hydrogen or a negative charge, and\n A \u03b8  is an anion, with the condition that n is zero when R 6\u2032  is a negative charge, and n is one when R 6\u2032  is hydrogen, \n comprising the steps of \n a) preparing a compound of formula \n wherein\n R 1 , R 2 , R 3  and R 4  are independently an amino protecting group or hydrogen with the condition that R 4  is not hydrogen if R 3  is hydrogen, or R 1  and R 2 , and/or R 3  and R 4  are bound together by a cyclic amino protecting group, \n R 5  is trialkylsilyl or hydrogen, \n R 6  is trialkylsilyl hydrogen or a negative charge, and \n A 1 \u25ef  is an anion, with the condition that n is zero when R 6  is a negative charge, and n is one when R 6  is trialkylsilyl or hydrogen, \n which comprises the steps of\n a-i) reacting a compound of formula \n \n with a silylating agent, optionally in presence of a catalyst, and with iodotrialkylsilane, a-ii) providing a compound of formula wherein R 1 -R 4  are as defined above, and optionally reacting this compound of formula IV with a silylating agent, a-iii) reacting the products of steps a-i) and a-ii), a-iv) and optionally desilylating the product of step a-iii) b) preparing a compound of formula wherein R 1 -R 4  and R 6\u2032  are as defined above, R 7  is hydrogen or an amino protecting group, R 10  is an ester protecting group, and A 2 \u2296  is an anion, with the condition that n is zero when R 6\u2032  is a negative charge, and n is one when R 6\u2032  is hydrogen, which comprises the step of reacting the compound of formula II with a compound of formula wherein R 7  and R 10  are as defined above, R 8  is Cl or SR9, wherein R 9  is C1-C6 straight or branched alkyl, C3-C6 cycloalkyl, or a substituted or unsubstituted mono- or bicyclic aryl or heteroaryl ring system of 5 to 12 atoms and where each monocyclic ring contains 0 to 3 hetero atoms, and each bicyclic ring contains 0 to 4 hetero atoms selected from N, O and S, and c) removing any protecting groups from the compound of formula V to produce a compound of formula I, d) if in the compound of formula I produced in step c) R 6\u2032  is a negative charge and n is zero optionally treating the compound of formula I produced in step c) with an acid to produce a compound of formula I, wherein R 6\u2032  is hydrogen and n is one, e) optionally exchanging the anion by a different anion in the compound of formula I produced in step d) or in the compound of formula I produced in step c) if R 6\u2032  is hydrogen and n is one.

Metadata:
- Claim Count in Document: 8.0
- Percentile: 88.0
- Lexical Diversity: 1.04
- Patent Class: 540.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15503564', '10695895', '10475845', '15319104', '14895809']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6291874607150506
- 35 USC 102 Novelty (BERT): 0.5121492428841644
- Combined Prediction Score: 0.617483638931962
- Mean Citation Score: 233.91299
- Max Citation Score: 239.83994
- Similarity Product: 161.44596902815226

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