- Synthetic method of nirudine hydrochloride
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The invention belongs to the field of medicine synthesis and discloses a synthetic method of hydrochloride. The synthesis method provided by the invention takes 2 - chloroethylamine as a raw material and is subjected to amine ester exchange. After the condensation reaction and the nitrification reaction, bendamustine hydrochloride is obtained. To the synthesis method of the hydrochloride, the toxicity of the reaction reagent is reduced, the safety of the synthesis process is improved, and the accuracy of the reaction yield calculation is improved. The synthesis method provided by the invention is suitable for synthesis of hydrochloride, and the synthesized hydrochloride is used for preparing hydrochloride for injection.
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Paragraph 0006; 0016; 0026-0028; 0033; 0035-0038; 0042-0044
(2021/08/25)
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- Structure-based drug design and potent anti-cancer activity of tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepines
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Judicial structural modifications of 5:7-fused ring-expanded nucleosides (RENs), based on molecular modeling studies with one of its known targets, human RNA helicase (hDDX3), led to the lead, novel, 5:7-5-fused tricyclic heterocycle (1). The latter exhibited promising broad-spectrum in vitro anti-cancer activity against a number of cancer cell lines screened. This paper describes our systematic, albeit limited, structure-activity relationship (SAR) studies on this lead compound, which produced a number of analogs with broad-spectrum in vitro anti-cancer activities against lung, breast, prostate, and ovarian cancer cell lines, in particular compounds 15i, 15j, 15m and 15n which showed IC 50 values in submicromolar to micromolar range, and are worthy of further explorations. The SAR data also enabled us to propose a tentative SAR model for future SAR efforts for ultimate realization of optimally active and minimally toxic anti-cancer compounds based on the diimidazo[4,5-d:4′, 5′-f][1,3]diazepine structural skeleton of the lead compound 1.
- Kondaskar, Atul,Kondaskar, Shilpi,Fishbein, James C.,Carter-Cooper, Brandon A.,Lapidus, Rena G.,Sadowska, Mariola,Edelman, Martin J.,Hosmane, Ramachandra S.
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p. 618 - 631
(2013/02/25)
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- Studies on novel 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones as potential TACE inhibitors: Design, synthesis, molecular modeling, and preliminary biological evaluation
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Compounds belonging to the class of 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones were synthesized and evaluated for their TACE inhibitory activity. Most of the compounds showed very good TACE inhibitory activity. Docking study clearly indicates importance of the P1′ group of the inhibitor for the TACE inhibitory activity. This work proves that these two classes of molecules could be used as potential leads for the development of TACE inhibitors.
- DasGupta, Shirshendu,Murumkar, Prashant R.,Giridhar, Rajani,Yadav, Mange Ram
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body text
p. 3604 - 3617
(2009/09/30)
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- Organosilicon synthesis of isocyanates: II. Synthesis of aliphatic, carbocyclic, and fatty-aromatic isocyanates
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Silylation of a series of aliphatic, carbocyclic, and fatty-aromatic amines gave the corresponding silyl derivatives whose yield depended on the electronic and steric structure of the substrate and the nature of the silylating agent. The yield of isocyanates obtained by phosgenation of the silyl derivatives under mild conditions decreased in going from aliphatic amines to benzylamines and rose as the length of the alkyl chain in fatty-aromatic amines extended. The most convenient procedure for the synthesis of low-boiling alkyl isocyanates was found to be based on the transformation of amines or ammonium salts into silyl or silyl silyl-carabamates, followed by pyrolysis of the latter in the presence of trichloro(phenyl)silane. Pleiades Publishing, Inc., 2006.
- Lebedev,Lebedeva,Sheludyakov,Ovcharuk,Kovaleva,Ustinova
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p. 469 - 477
(2008/02/07)
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- SYNTHESIS, STRUCTURE, AND ANTITUMOR ACTIVITY OF 5-SUBSTITUTED 5--2,2-DIMETHYL-1,3-DIOXANES
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5-Substituted 5--2,2-dimethyl-1,3-dioxanes were synthesized by the nitrosation of 5-substituted 5--2,2-dimethyl-1,3-dioxanes by sodium nitrite in 50percent aqueous acetic acid or by N2O3 in chloroform.Nitrosation takes place regioselectively, irrespective of the method.
- Kon'kov, S. A.,Kraiz, B. O.,Shenberg, N. N.,Gindin, V. A.,Stukov, A. N.,et al.
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p. 2092 - 2097
(2007/10/02)
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- Imidazolidinones as brain activators
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This invention relates to imidazolidinone compounds of the formula STR1 wherein Q is methylene group or a single bond: R is a heterocyclic group selected from the group consisting of pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl and 1,3-thiazolyl which may be unsubstituted or with a substituent selected from the group consisting of lower alkyl, lower alkoxy and halogen atom, wherein R is bonded to Q or, when Q is a single bond, to the imidazolidinone ring, through the carbon atom of R; the ring A is an unsubstituted phenyl or a substituted phenyl having 1 or 2 substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, lower alkylthio, trihalogeno-lower alkyl and nitro; Y is vinylene group or ethynylene; m is a integer from 1 to 6 and n is 0, 1 or 2, or a pharmacetically acceptable salt thereof. These compounds aer useful as cerebral activators, anti-depressants and nootropic drugs.
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