- Antibacterial Activities of Transition Metal complexes of Mesocyclic Amidine 1,4-diazacycloheptane (DACH)
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The titled compound 1,4-diazacycloheptane have vibrational freedom which allows it to coordinate to metal through 1st and 4th positions. Copper (II) and Nickel (II) complexes of DACH were prepared and characterized through UV-Visible, FT-IR, elemental analyses, conductance, and magnetic susceptibilities and compared to the results published in Inorg. Chem., 8(3), 528 (1969). The prepared complexes bearing different coordinating or non-coordinating anions were screened against four different pathogenic bacterial strains to study anionic effect on antibacterial activity. The MIC values of all the compounds suggest that [Cu(DACH)2Br2] is almost inactive against the tested microbes except Staph aureus. Rest of the metal complexes are active at their respective MIC values.
- Rehman, Sadia,Ikram, Muhammad,Subhan, Fazle,Sinnokrot, Mutasem,Khan, Waliullah
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- Unconventional Synthetic Process of Fasudil Hydrochloride: Costly Homopiperazine Was Avoided
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An efficient, robust, and cost-effective synthetic process of fasudil hydrochloride 1 was developed. Starting from readily available ethylenediamine and 5-isoquinoline sulfonyl chloride, the target product 1 was prepared through a six-step reaction, including sulfonamidation, protection, nucleophilic substitution, deprotection, cyclization, and salification. The process afforded 1 in 67.1% overall yield (based on 5-isoquinoline sulfonyl chloride) with 99.94% purity. Compared to the earlier published methodologies, the use of homopiperazine or its derivatives as intermediates was avoided. The salient features of this environmentally friendly synthetic route include easily available starting materials and operational simplicity, which could be suitable for large-scale industrial production.
- Niu, Jinming,Wang, Dingding,Wu, Weiting,Yang, Wu-Lin,Zhao, Jianhong
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- A cardiovascular drug fasudil hydrochloride intermediate simple synthesis of process
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The invention discloses a cardiovascular drug fasudil hydrochloride intermediate simple synthesis process, taking ethylenediamine, BOC anhydride, DCM into the reaction bottle stirring, GC to intermediate state the reaction is complete, the reaction solution is concentrated under reduced pressure, concentrate, tetrahydrofuran to stir until completely dissolved, addition of sodium methoxide, thermal insulation stirring [...] 1, 3 - dibromo propane, thermal insulation to stir until the reaction is complete, the reaction solution is poured into ice water, extracted with ethyl acetate twice, combined with the organic phase, a washed, dried with anhydrous sodium sulfate, concentrated under reduced pressure to dry, taking concentrated intermediate, 40% sodium hydroxide, ethanol into the reaction bottle stirring, the reaction solution is heated to reflux, thermal insulation reaction to intermediate state hydrolysis, reverse the ice water, for two armor uncle ether extraction, the combined organic phase, a washed, dried with anhydrous sodium sulfate, concentrated under reduced pressure to dry, adding hexane stirring crystallization, to obtain the product, yield 87.0%, GC99%, raw materials of this invention is simple and easy, the product has high purity, simple and convenient operation, the work efficiency is high.
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Paragraph 0021; 0022
(2019/05/15)
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- A method of preparing high-piperazine
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The invention discloses a preparation method of homopiperzine. The preparation method comprises the following steps: by taking ethylene diamine as a raw material, performing acylation reaction on ethylene diamine and toluenesulfonyl chloride in an n-butyl alcohol solvent to prepare N, N'-dipara-toluene sulfonyl ethylene diamine; directly performing ring-closure reaction on N, N'-dipara-toluene sulfonyl ethylene diamine which does not need to be separated from a reaction liquid and chlorobromide under the action of sodium hydroxide to prepare N, N'-dipara-toluene sulfonyl homopiperzine; removing sulfonyl under the action of hydrobromic acid and phenol to obtain homopiperzine hydrobromide; finally, dissociating with sodium hydroxide and bringing water from toluene to obtain high-purity homopiperzine. The production method is simple to operate, cost-saving, convenient for large-scale production, and can be preparing high-purity high-yield homopiperzine.
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Paragraph 0029; 0034; 0039; 0044; 0045; 0049; 0054
(2017/10/07)
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- Method for preparing homopiperazine by utilizing ethyl trifluoroacetate
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The invention discloses a method for preparing homopiperazine by utilizing ethyl trifluoroacetate. The method comprises the following steps: (1) taking ethylenediamine as an initial raw material; enabling the ethylenediamine to react with the ethyl trifluoroacetate under the action of an organic solvent, so as to prepare bistrifluoroacetylethylenediamine; (2) enabling the bistrifluoroacetylethylenediamine obtained by the step (1) to react with a 1,3-disubstituted propane compound under the action of a solvent and a catalyst, so as to obtain bistrifluoroacetyl homopiperazine; (3) enabling the bistrifluoroacetyl homopiperazine obtained by the step (2) to react with a hydrogen chloride ethanol solution to obtain homopiperazine bihydrochloride; recycling the ethyl trifluoroacetate; (4) enabling the homopiperazine bihydrochloride obtained by the step (3) to react with alkali under the action of a solvent and a catalyst, so as to prepare the homopiperazine. The method disclosed by the invention has the beneficial effects of simplicity and convenience for operation, relatively low cost, relatively high yield, relatively small pollution and wide applicable range, and can meet the requirements on industrial production of products.
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Paragraph 0067; 0078-0084; 0086; 0087
(2017/07/21)
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- Absorption medium and method for removing sour gases from fluid streams, in particular from flue gases
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Absorption medium for acid gases comprising an oligoamine (A) of the general formula (I) and a primary or secondary alkanolamine (B) of the general formula (II) in which the weight ratio of oligoamine (A) to the primary or secondary alkanolamine (B) is 0.2 to 4, and also the process for removing acid gases from a gas stream by contacting the gas stream at a pressure of 0.05 to 10 MPa abs with an aqueous solution brought to and maintained at a temperature of 20 to 80° C. of said absorption medium.
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- TRANSAMINATION OF NITROGEN-CONTAINING COMPOUNDS TO MAKE CYCLIC AND CYCLIC/ACYCLIC POLYAMINE MIXTURES
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A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses.
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Page/Page column 18-20
(2012/05/31)
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- DIARYLALKYL CYCLIC DIAMINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS
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Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-la and/or MCP-l on target cells, and are useful as a therapeutic drug and/or preventative drug in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.
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- Pyridyl-and pyrmidyl-piperazines useful for the treatment of mental disorders
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The present invention concerns novel compounds of the general formula; STR1 wherein R 1 is halogen or hydrogen and R 2 is halogen; X is either oxygen, sulfor or methyleneR 3 and R 4 are the same or different and selected from hydrogen and lower alkyl;n is 2 or 3;A is selected from the following pyrimidyl or pyridyl groups STR2 wherein R 5 is selected from hydrogen, lower alkyl or halogen; R 6 and R 7 are the same or different and selected from hydrogen, halogen, lower alkyl, electron donor groups such as lower alkoxy or hydroxy, electron acceptor groups such as cyano, nitro, trifluoromethyl, COOR 8, CONR 9 R 10 or CO-B;wherein R 8 is hydrogen or lower alkyl;R 9 and R 10 are the same or different and selected from hydrogen, lower alkyl and cycloalkyl;B is selected from STR3 wherein m is 1, 2, 3 or 4. R 11 is selected from hydrogen or lower alkyl, and the pharmacologically active salts thereof.The new compounds are useful for treating mental disorders.
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- Pharmaceutical compositions of N-heterocyclic benzenesulfonamides and their use
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The invention relates to new N-cyclic benzenesulfonamides, their process of preparation and their use as active substance of pharmaceutical compositions. The new benzenesulfonamides according to the invention correspond to the following general formula (I): STR1 in which: V represents, for example, hydrogen, W represents, for example CF3, X represents, for example, hydrogen, Y represents, for example, hydrogen, n is 2 or 3, Z represents, for example, the group NR4, in which R4 represents, for example, hydrogen. These compounds are useful in pharmaceutical compositions for the treatment of nervous disorders with anxiety.
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- Novel polytriazine compounds
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Novel tetraalkyl piperidine radical containing polytriazine compounds are produced by reacting a dihalogen-triazine with a bifunctional compound containing amine, alcohol, mercaptan or phenol groups at least one of the bifunctional compounds containing a tetraalkyl piperidine radical. The compounds are valuable light stabilizers for synthetic polymers, particularly polyolefin in the form of fibers or films.
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