- Method for synthesizing p-methoxybenzyl [3-(aminomethyl)-oxetane-3-yl]carbamate p-chlorobenzoate
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The invention provides a method for synthesizing p-methoxybenzyl [3-(aminomethyl)-oxetane-3-yl]carbamate p-chlorobenzoate. The method comprises the following steps: a, preparing a compound 2 from a cyclic imido group substituted compound 1, wherein the cyclic imido group is any one of phthalimide, succimide and maleimide; b, carrying out an amination reaction on a primary amine and the compound 2to generate a compound 3; and c, reacting the compound 3 with 4-chlorobenzoic acid to obtain a compound 4. A reaction route is shown in the description. The synthesis method is friendly to the environment, and is suitable for large-scale industrial production.
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Paragraph 0046; 0047
(2018/05/30)
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- SUBSTITUTED PYRAZOLOAZEPIN-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
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Page/Page column 117; 118
(2018/07/05)
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- Synthesis of novel 3-(4-substitutedaryloxymethyl) oxetan-3- ylamines
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2,2-Bis (bromomethyl) propane-1,3-diol (1) was cyclized in the presence of sodium ethoxide at room temp to obtain (3-(bromomethyl) oxetan-3-yl) methanol (2) which was treated with various phenols (3) to yield (3-(aryloxymethyl) oxetan-3-yl) methanol (4). The latter, on oxidation with KMnO4 in aq. NaOH containing dioxan gave the corresponding carboxylic acid derivatives 5.5 with benzyl alcohol containing Diphenyl Phosphoryl Azide (DPPA) gave 3-(4-substitutedaryloxymethyl) oxetan-3-ylamines (7) via N-CBz protected aminooxetanes (6).
- Shyamsunder Reddy,George Vineel,Naidu,Dubey
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p. 345 - 348
(2019/01/21)
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- NOVEL POLYMERIC PHOTOINITIATORS AND PHOTOINITIATOR MONOMERS
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The present invention provides polymeric photoinitiators being co-polymers of photoinitiator monomers and at least one further monomer, as well as the photoinitiator monomers being intermediates in the preparation of such polymeric photoinitiators. Additi
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Page/Page column 89
(2013/12/03)
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- Synthesis of 3,3-disubstituted oxetane building blocks
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The synthesis of two different sets of 3,3-disubstituted oxetane building blocks is described. These molecules can be usefully incorporated in more complex structures to modulate their metabolic and physicochemical properties. The synthetic pathways are g
- Vigo, Daniele,Stasi, Luigi,Gagliardi, Stefania
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scheme or table
p. 565 - 567
(2011/03/18)
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- 1,1-DIOXO-1-THIA-5,10-DIAZADIBENZOCYCLOHEPTENES USEFUL AS HEPATITIS C VIRUS INHIBITORS
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Inhibitors of HCV replication of formula (I) the stereoisomers, prodrugs, tautomers, racemics, salts, hydrates or solvates thereof wherein R1a; R1b R2; R3; R4a and R4b have the meaning defi
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Page/Page column 157-158
(2008/12/08)
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- Chemical transformation of 3-bromo-2,2-bis(bromomethyl)-propanol under basic conditions
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The mechanism of the spontaneous decomposition of 3-bromo-2,2- bis(bromomethyl)propanol (TBNPA) and the kinetics of the reaction of the parent compound and two subsequent products were determined in aqueous solution at temperatures from 30 to 70 °C and pH from 7.0 to 9.5. TBNPA is decomposed by a sequence of reactions that form 3,3-bis(bromomethyl)oxetane (BBMO), 3-bromomethyl-3-hydroxymethyloxetane (BMHMO), and 2,6-dioxaspiro[3.3]-heptane (DOH), releasing one bromide ion at each stage. The pseudo-first-order rate constant of the decomposition of TBNPA increases linearly with the pH. The apparent activation energy of this transformation (98 ± 2 KJ/mol) was calculated from the change of the effective second-order rate constant with temperature. The pseudoactivation energies of BBMO and BMHMO were estimated to be 109 and 151 KJ/mol, respectively. Good agreement was found between the rate coefficients derived from changes in the organic molecules concentrations and those determined from the changes in the Br- concentrations. TBNPA is the most abundant semivolatile organic pollutant in the aquitard studied, and together with its byproducts they posess an environmental hazard. TBNPA half-life is estimated to be about 100 years. This implies that high concentrations of TBNPA will persist in the aquifer long after the elimination of all its sources.
- Ezra, Shai,Feinstein, Shimon,Bilkis, Itzhak,Adar, Eilon,Ganor, Jiwchar
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p. 505 - 512
(2007/10/03)
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- Process and intermediate products for the production of 5-oxaspiro [2.4]heptan-6-one
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5-Oxaspiro[2.4]heptan-6-one: STR1 is obtained from [3-(hydroxymethyl)oxetan-3-yl]acetonitrile by reaction with hydrogen bromide and then cyclizing the intermediate product 4,4-bis(bromomethyl)dihydro-2-furanone with zinc. 5-Oxaspiro[2.4]heptan-6-one is an intermediate product for the production of leukotriene antagonists.
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- 3-Azidomethyl-3-nitratomethyloxetane
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3-Azidomethyl-3-nitratomethyloxetane, a novel oxetane compound, is used as a monomer for the formation of homopolymers and copolymers with other known energetic oxetane monomers. The polyethers of the present invention can be subsequently cured to form elastomers suitable for use as energetic binders in propellant formulations or the like.
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- Polymers and copolymers from 3-azidomethyl-3-nitratomethyloxetane
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3-Azidomethyl-3-nitratomethyloxetane, a novel oxetane compound, is used as a monomer for the formation of homopolymers and copolymers with other known energetic oxetane monomers. The polyethers of the present invention can be subsequently cured to form elastomers suitable for use as energetic binders in propellant formulations or the like.
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- Process for preparing azetidine derivatives and intermediates thereof
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The invention provides a process for preparing azetidine-3-carboxylic acid or salts thereof; useful as chemical hybridizing agents, which comprises treating a compound of the formula STR1 wherein R represents a hydrogen atom or a group of formula R1 R2 CH-- wherein R1 and R2 are independently selected from hydrogen, alkyl or optionally substituted phenyl moieties, with nitric acid and subjecting the resulting initial product to acid conditions to produce an acid-addition salt of azetidine-3-carboxylic acid, and thereafter, if desired, converting the acid-addition salt to the free acid or another salt of the acid, 1-nitrosoazetidine-3,3-dicarboxylic acid, 1-nitrosoazetidine-3-carboxylic acid and salts thereof being intermediates in the process.
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