- Optimisation by design of experiment of benzimidazol-2-one synthesis under flow conditions
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A novel flow-based approach for the preparation of benzimidazol-2-one (1) scaffold by the 1,10-carbonyldiimidazole (CDI)-promoted cyclocarbonylation of o-phenylenediamine (2) is reported. Starting from a preliminary batch screening, the model r
- Mostarda, Serena,Maz, Tug?e Gür,Piccinno, Alessandro,Cerra, Bruno,Banoglu, Erden
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- Method for preparing carbonyl heterocyclic compound
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The invention provides a method for preparing a carbonyl heterocyclic compound, wherein Lewis base and hydrosilane are used as accelerators and can efficiently enable an ortho-substituted aniline compound to react with normal-pressure CO2 to generate corresponding carbonyl heterocyclic compounds containing different functional groups under mild conditions (100 DEG C, digital). According to the method, normal-pressure CO2 is used as an environmentally-friendly non-toxic carbonylation reagent, and cheap Lewis base and PMHS (industrial silicon waste) are used as accelerators, so that the use of CO, high-pressure CO2 and noble metal catalysts is avoided, the intermediate isocyanate does not need to be purified and separated, the pure product can be obtained only through simple suction filtration and separation after the reaction is finished, and the synthetic method is efficient and universal, is suitable for preparing a series of benzimidazolone, benzoxazolone and benzothiazolone compounds and has high industrial application value.
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Paragraph 0054-0059; 0078-0083
(2020/03/25)
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- A 5-acetoactylaminobenzimidazolon preparation method (by machine translation)
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The present invention provides a 5-acetoactylaminobenzimidazolon preparation method, comprising the following steps: under the action of the acid catalyst, will 5-amino-benzimidazolone, double-ketene, alcohol and water to the reaction, the 5-acetoactylaminobenzimidazolon; the alcohol is methanol, ethanol and propanol in one or several kinds of. The present invention provides a method of preparing 5-acetoactylaminobenzimidazolon in the production process, the reaction temperature of the acetylation process, thus reducing the equipment requirements, and also reducing the risk of the coefficient in the actual production, the mild reaction conditions, is easy to operate. (by machine translation)
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Paragraph 0048
(2017/02/17)
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- Au catalyzed synthesis of benzimidazoles from 2-nitroanilines and CO 2/H2
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The gold-catalyzed synthesis of benzimidazoles from 2-nitroanilines and CO2 in the presence of H2 was reported, and a series of benzimidazoles were obtained under relatively mild conditions. Several supported Au catalysts including Au/TiO2, Au/Al2O3, Au/ZnO, Au/polyurea and Au/hydrotalcite were examined for the synthesis of benzimidazole from the reaction of 2-nitroaniline with CO2 and H 2, among which Au/TiO2 displayed the best performance. The reaction mechanism was investigated, and it was found that the production of benzimidazole underwent the formation of o-phenylenediamine via the hydrogenation of 2-nitroaniline, followed by the cyclization of o-phenylenediamine with CO2 and H2. This work provides a CO2-involved route for the synthesis of benzimidazoles, which may widen the applications of CO2 in the chemical synthesis. This journal is the Partner Organisations 2014.
- Hao, Leiduan,Zhao, Yanfei,Yu, Bo,Zhang, Hongye,Xu, Huanjun,Liu, Zhimin
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p. 3039 - 3044
(2014/06/10)
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- Samarium diiodide mediated regeneration of 1,2-benzenediamine and preparation of benzimidazolin-2-ones from 2,1,3-benzothiadiazoles
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On treatment with Sml3 in THF and in the presence of methanol, 2,1,3-benzothiadiazoles underwent reductive N-S bond cleavage leading to 1,2-benzenediamines in high yields. Without methanol but in the presence of triphosgene, benzimidazolin-2-ones were obtained in moderate yields under mild conditions.
- Fan, Xuesen,Zhang, Xinying,Zhang, Yongmin
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- Substituted amino methyl factor Xa inhibitors
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The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Method for manufacturing pigment dispersed liquid, and pigment dispersed liquid, and ink for ink-jet printer recording using said pigment dispersed liquid
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A method for manufacturing a pigment dispersed liquid, comprising at least: Step A of introducing a hydrophilic dispersibility-imparting group directly and/or via another atomic group to the surface of pigment particles; Step B of dispersing the pigment o
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- Compounds useful in therapy
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There is provided a compound of formula I, wherein Het1, T, X, R1, R2and R3have meanings given in the description, which are useful in the prophylaxis and in the treatment of diseases mediated by opiate receptors, such as pruritus.
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- Heteroaryl-phenyl substituted factor Xa inhibitors
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The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.
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- Heteroaryl- phenyl heterobicyclic factor Xa inhibitors
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The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Use of compounds for the elevation of pyruvate dehydrogenase activity
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The use of compounds of the formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs: wherein: Ring C is phenyl or a carbon linked heteroaryl ring substituted as defmed within; R1is an ortho substituent as defined within; n is 1 or 2; A—B is a linking group as defined within; R2and R3are as defined within; R4is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.
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- Method of acylating amines using N,N'-diacylimidazolone derivatives
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The present invention provides a method of acylating organic amines using N,N'-diacylimidazolone derivatives represented by the general formula I as follows: STR1 wherein R1 and R2 are the same or different, which are selected from t
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- SEROTONERBIC TETRAHYDROPYRIDOINDOLES
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This invention provides novel, optionally substituted tetrahydropyridoindoles which are useful serotonergic agents for the treatment of central nervous system disorders.
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- Process for the preparation of cyclic ureas
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A process for the preparation of cyclic urea derivatives of the formula STR1 in which R1 and R2 are equal or different and represent hydrogen, alkyl having from 1 to 6 carbon atoms or alkoxy having from 1 to 3 carbon atoms, which comprises reacting a 1,2-diaminobenzene of the formula STR2 in which R1 and R2 have the meaning indicated above are reacted with carbon dioxide in the presence of water under superatmospheric pressure at a temperature of at least 120° C.
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- Method of producing benzimidazolone
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A method of producing benzimidazolone which comprises reacting a feed compound having the general formula STR1 wherein X and Y independently represent an amino group or a nitro group, with carbon monoxide in solvent in the presence of selenium and a base, and in the presence of water when the feed compound has nitro groups.
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- Process for the manufacture of benzimidazolones-(2)
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Process for the manufacture of benzimidazolones-(2) wherein an o-phenylenediamine is reacted with optionally alkylated urea in the ratio of 1 to 1.3 moles per mole o-phenylenediamine in an organic solvent which has a solubility in water of not more than 5 g/l and has a boiling point above 100° C, at a temperature between 100° and 200° C.
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- Process for preparing 2-benzimidazolones
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This invention is directed to a process for preparing 2-benzimidazolone which comprises reacting 2'-carbamoylphthalanilic acid in an alkaline medium with a metal hypohalite.
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