- METHOD OF MANUFACTURING BIPHENYLDICARBOXYLIC ACID
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A method for producing biphenyldicarboxylic acid according to example embodiments of the present invention is to react a biphenyl (biphenyl) with an acyl halide (acyl halide) - based compound to form an agent 1 intermediate. 1 Intermediate and 3 nd amine-based compound are reacted to form a 2 intermediate, and the step 2 intermediate is base-treated. 4,4 ' - Biphenyldicarboxylic acid can be efficiently produced.
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Paragraph 0101-0106
(2021/05/25)
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- Micro-electro-flow reactor (μ-EFR) system for ultra-fast arene synthesis and manufacture of daclatasvir
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The World Health Organization (WHO) has listed daclatasvir (DCV), symmetrical arene, as one of the essential medicines for human health. DCV manufacturing is usually carried out in a non-continuous or "batch" approach over multiple locations and is severely limited by long production times (3-10 days), resulting in non-affordability (highly expensive) and disruption of the potential chain supply. Here, we report the total process system including the development of a novel electro-flow reactor containing patterned electrodeposited Ni or Pt nanoparticles over a copper electrode for a C-C coupling reaction in a co-reductant/oxidant-free, ultra-fast process for symmetrical substituted/unsubstituted biphenyl synthesis. This method was further extended to a new generation commercial batch synthetic route for continuous flow ultra-fast daclatasvir synthesis in 33.2 min. We envisage that this micro-electro-flow reactor (μ-EFR) system platform will substantially enable advances in continuous-μ-flow fine chemical manufacturing, multistep reaction sequences, reaction devising equipment, and real-time extraction.
- Mahajan, Bhushan,Mujawar, Taufiqueahmed,Ghosh, Subhash,Pabbaraja, Srihari,Singh, Ajay K.
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p. 11852 - 11855
(2019/10/11)
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- Industrial production method for Daclatasvir key intermediate
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The invention relates to the technical field of biochemical engineering and specifically relates to an industrial production method for a Daclatasvir key intermediate 5,5'-[1,1'-biphenyl]-4,4'-diyl di[2-(2S)-2-pyrrolidyl-1H-imidazole]terthydrochloride. Th
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Paragraph 0025-0032; 0047-0054
(2019/04/04)
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- Design, synthesis, and biological evaluation of a new series of biphenyl/bibenzyl derivatives functioning as dual inhibitors of acetylcholinesterase and butyrylcholinesterase
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Alzheimer's disease (AD), the most common form of dementia in adults, is a progressive neurodegenerative disorder of the brain characterized by loss of memory and steady deterioration of cognition. Here, a series of symmetrical molecules containing biphenyl/bibenzyl scaffolds (12-36) were designed, synthesized, and evaluated for their ability to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A biological evaluation showed that most of these biphenyl derivatives were potent AChE and BuChE inhibitors. Among them, compound 15 displayed the greatest ability to inhibit BuChE (IC50 = 0.74 μM) and was also a good AChE inhibitor (IC50 = 1.18 μM). Compound 19 was not only a potent AChE inhibitor (IC50 = 0.096 μM), but also a mild BuChE inhibitor (IC50 =1.25 μM). Overall, these results suggested that compound 19 may be a promising agent in the treatment of AD.
- Wang, Dong-Mei,Feng, Bo,Fu, Hui,Liu, Ai-Lin,Wang, Lin,Du, Guan-Hua,Wu, Song
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- DACLATASVIR FREE BASE AND PROCESS FOR THE PREPARATION THEREOF
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The present invention relates to daclatasvir free base, processes for its preparation, a process for its conversion into pharmaceutically acceptable salts of daclatasvir. The present invention also relates to a process for the preparation and purification
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Page/Page column 22
(2017/03/08)
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- Preparation method and application of 4,4'-dihalide acetodiphenyl
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The invention relates to a preparation method of 4,4'-dihalide acetodiphenyl and an application of 4,4'-dihalide acetodiphenyl in synthesis of a Daclatasvir intermediate. The raw materials of biphenyl and a halogen acetylation reagent have the advantages of low cost and easy acquisition; the Daclatasvir intermediate is synthesized by 4,4'-dihalide acetodiphenyl through a one kettle way, the processes are simplified, and the reaction yield is greatly increased.
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Paragraph 0046; 0047; 0048
(2017/07/21)
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- The b, butyrylcholinesterase with double-inhibiting active compound
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The invention provides an inhibitor of acetylcholine esterase and cholinesterase shown in the general formula (I), wherein R1, R2 and N form an aliphatic heterocyclic ring with 3-7 carbons containing 1-2 hetero atoms, and X is selected from a covalent bon
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Paragraph 0061
(2017/01/02)
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- Synthesis of (2-hydroxo-5-chlorophenylaminoisonitrosoacetyl)phenyl ligands and their complexes: Spectral, thermal and solvent-extraction studies
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Four different types of new ligands Ar[COC(NOH)R] n (Ar=biphenyl, n = 1 H2L1; Ar=biphenyl, n = 2 H 4L2; Ar=diphenylmethane, n = 1 H2L3; Ar=diphenylmethane, n = 2 H4L4; R=2-amino-4-chlorophenol in all ligands) have been obtained from 1 equivalent of chloroketooximes Ar[COC(NOH)Cl] n (HL1-H2L4) and 1 equivalent of 2-amino-4-chlorophenol (for H2L1 and H 2L3) or 2 equivalent of 2-amino-4-chlorophenol (for H 4L2 and H4L4). (Mononuclear or binuclear cobalt(II), nickel(II), copper(II) and zinc(II) complexes were synthesized with these ligands.) These compounds have been characterized by elemental analyses, AAS, infra-red spectra and magnetic susceptibility measurements. The ligands have been further characterized by 1H NMR. The results suggest that the dinuclear complexes of H2L1 and H2L3 have a metal:ligand ratio of 1:2; the mononuclear complexes of H4L2 and H4L4 have a metal:ligand ratio of 1:1 and dinuclear complexes H4L2 and H4L4 have a metal:ligand ratio of 2:1. The binding properties of the ligands towards selected transition metal ions (Mn II, CoII, NiII, CuII, Zn II, PbII, CdII, HgII) have been established by extraction experiments. The ligands show strong binding ability towards mercury(II) ion. In addition, the thermal decomposition of some complexes is studied in nitrogen atmosphere.
- Karipcin, Fatma,Dede, Bülent,Cengiz, Mustafa
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experimental part
p. 530 - 540
(2010/08/04)
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