PATENT CLAIM ANALYSIS

Application Number: 16280534
Application Type: Utility
Filing Date: 2019-02
Publication Date: 2019-06
Patent Classification: ["514", "340000"]

Abstract:
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.

Claim (Index 3):
A process to prepare compound of formula VI* or VIa*, or a mixture thereof: comprising (i) reacting ester 6, with morpholine to provide morpholine amide 7: (ii) reacting morpholine amide 7: to provide ketone 3, (iii) performing olefination of ketone 3, to provide olefin 2-5, (iv) reacting olefin 2-5, under asymmetric dihydroxylation conditions to provide a compound of formula 2-6b or 2-7d, or a mixture thereof;\n (v) activating the primary alcohol of 2-6b or 2-6d to provide VI* or VIa \n or a mixture thereof;\n wherein M is Mg or MgX; and X is halogen; \n the asymmetric dihydroxylation conditions comprise: \n (i) AD-mix alpha or AD-mix beta; or \n (ii) a first oxidant in catalytic amount selected from OsO 4  or K 2 OsO 2 (OH) 4 ; \n (iii) a second oxidant in stoichiometric amount selected from K 3 Fe(CN) 6  or N-methylmorpholine-N-oxide; \n (iv) a base selected from NaHCO 3 , Na 2 CO 3 , Cs 2 CO 3 , or K 2 CO 3 ; and \n (v) a chiral ligand that is selected from (DHQ) 2 PHAL, (DHQD) 2 PHAL, (DHQD) 2 AQN, (DHQ) 2 AQN, (DHQD) 2 PYR, and (DHQ) 2 PYR; and \n each R 1  is independently, halo or \n each Y 1  is independently \u2014OH, \u2014OSO 2 -substituted alkyl, \u2014OSO 2 -aryl, \u2014OSO 2 -substituted aryl, \u2014O(C\u2550O)-alkyl, \u2014O(C\u2550O)-substituted alkyl, \u2014O(C\u2550O)-aryl, \u2014O(C\u2550O)-substituted aryl, or halogen; and each R 12  is independently H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted hetrocyclyl.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 99.0
- Lexical Diversity: 1.22581
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15126392', '16280527', '16030228', '15126420', '15126359']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.793905810640508
- 35 USC 102 Novelty (BERT): 0.5383257788722291
- Combined Prediction Score: 0.7683478074636801
- Mean Citation Score: 329.59696
- Max Citation Score: 374.94827
- Similarity Product: 311.16280749865945

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