- Preparation method of 2-chlorethamin hydrochloride
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The invention discloses a preparation method of 2-chlorethamin hydrochloride. The method concretely comprises the following steps of using neovaricaine as raw materials; using organic acid as a catalyst; using chlorine hydride as a chlorination agent for preparing the 2-chlorethamin hydrochloride through substitute reaction. The method provided by the invention has the advantages that the raw materials can be easily obtained; the reaction speed is high; the product yield and the purity are high; byproducts of chlorine hydride are used as a chloro reagent for replacing thionyl chloride; the generation of pollution gas is avoided; the environment pollution is greatly reduced.
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Paragraph 0017; 0018; 0019; 0020-0032
(2018/06/16)
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- Novel synthesis method of Istaroxime
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The invention belongs to the field of pharmaceutical chemistry, and discloses a novel synthesis method of Istaroxime. The method comprises the following steps: by using dehydrogenated epiandrosterone as an initial raw material, carrying out epoxidation, ring opening, reduction, oxidation and other reactions to prepare an intermediate M-06; by using ethyl benzoate as an initial raw material, reacting the ethyl benzoate with hydroxylamine hydrochloride to obtain phenyl hydroximic acid, carrying out hydrochlorination and chlorination by using ethanolamine as a raw material to obtain dichloroacetate, and carrying out substitution, hydrolysis and other reactions on the dichloroacetate and the phenyl hydroximic acid to obtain an intermediate M-11; and finally, reacting the M-06 with the M-11 to obtain the end product Istaroxime. According to the method, in the intermediate M-06 synthesis process, the polarity of all the intermediates has great differences from that of the impurities and reaction reagents; and in the intermediate 11 synthesis process, the active spots capable of participating in the chemical reaction in the reaction substrate are simple. Therefore, the method can achieve the requirements without carrying out column chromatography purification, thereby simplifying the synthesis after-treatment process.
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Paragraph 0111; 0112; 0113; 0114
(2016/10/10)
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- Side chain impacts on pH- and thermo-responsiveness of tertiary amine functionalized polypeptides
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The systemic investigation of the structural impacts of side chains on the pH- and thermo-responsiveness of tertiary amine functionalized poly(l-glutamate)s (TA-PGs) was carried out. The TA-PGs polymers were effectively synthesized by Cu(I)-catalyzed azide-alkyne cycloaddition click reaction of azido tertiary amines with poly(γ-propargyl-l-glutamate) (PPLG). Turbimetric measurements were performed to characterize the pH- and temperature-induced phase transition of TA-PGs in aqueous solution, which suggested a structural dependence of the properties on the N-substituted groups and the "linkers" between 1,2,3-triazole ring and the tertiary amine groups in the side chains. In detail, the pH responsive properties of TA-PGs were basically determined by the hydrophobicity of the N-substituted groups in the side chains and the pH transition point (pHt) decreased as the increasing hydrophobicity of the N-substituted groups, while the temperature-responsiveness of TA-PGs were affected by either the N-substituted groups or the "linkers." TA-PGs with a moderate N-substituted amine group (e.g., DEA, PR, and PD) or a branched "linker" (e.g., iso-propylene and 2-methylpropylene group) were more likely to express the LCST-type phase transition tuned by pH variation. These structure-property relationships revealed in this study would help to develop the applications of TA-PGs in smart drug delivery systems. Copyright
- Xiao, Chunsheng,Cheng, Yilong,Zhang, Yu,Ding, Jianxun,He, Chaoliang,Zhuang, Xiuli,Chen, Xuesi
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p. 671 - 679
(2014/02/14)
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- Synthesis of some nitrogen mustards (Mannich bases)
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Several Mannich base half nitrogen mustards have been synthesised by the condensation of 3-substituted phthalimides and 4-substituted phthalimides with (2-chloroethyl) amine in ethanol- formalin.
- Sinha, Girish Kumar,Mehra,Kumar, Sharad
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experimental part
p. 1261 - 1264
(2012/04/04)
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- Synthesis and structure-activity relationships of juvenoids derived from 2-(4-hydroxybenzyl)cycloalkan-1-ones
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Juvenoids 16-30, 32, 36, 38-41, 44-46, and 49-56 containing carbamate, carbonate, and urea moieties in the molecule were synthesized and subjected to a biological screening. Carbamate juvenoids 1-4 were used as reference compounds for a detailed structure-activity study of their analogues. A clear relationship between the nature of the side chain functional group and the biological activity was found. Surprisingly, not only the juvenoids 1,4 but also 38-41, the compounds with a reversed carbamate N,O-substitution pattern, showed very promising biological activity. In contrast, the carbonate and urea derivatives displayed a remarkably low activity. The relationship between the size and substitution at atoms C(2) and C(3) of the saturated ring and the biological activity is very complex and is still not completely understood.
- Rejzek,Wimmer,Saman,Ricankova,Nemec
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p. 1241 - 1255
(2007/10/02)
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- CHIMIE DES RADIOPROTECTEURS: REVISION DE LA SYNTHESE DES ACIDES S- ET S-PHOSPHOROTHIOIQUES
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Simple, reproducible and detailed preparations of S- and S- phosphorothioic acids (HO)2P(O)-S-(CH2)2-NH-(CH2)3-NH-R (R=H and CH3), named WR 2721 and WR 1680 respectively, are described.The yields of each step have been optimized to facilitate the synthesis of these compounds of large interest in the cancer radio- and chemotherapy.
- Laduranty, Joelle,Lion, Claude,Mesnard, Daniele,Miginiac, Leone
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p. 903 - 912
(2007/10/02)
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- Reactions of Copper(II) with Ligands Containing Thioether Donors
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Preparations of three ligands containing thioether donor atoms are detailed and their interactions with cupric ions discussed.The affinity of these sulfur donors for copper(II) is small, and stable complexes can only be formed under restricted solvent and anion conditions.
- Braithwaite, Andrew C.,Rickard, Clifton E. F.,Waters, T. Neil
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p. 2665 - 2669
(2007/10/02)
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- Process for producing sulfonylamides
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Sulfonylamide derivatives of the formula, wherein R is an alkyl or a phenyl group, which are particularly useful for the production of photographic chemicals, are prepared by the reaction between a sulfonylhalide of the formula, wherein R is as defined above, and X is chlorine or bromine, and 2-chloroethylamine or its salt, which is prepared by the chlorination of monoethanolamine with thionylchloride.
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