870-24-6Relevant articles and documents
Preparation method of 2-chlorethamin hydrochloride
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Paragraph 0017; 0018; 0019; 0020-0032, (2018/06/16)
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.
Side chain impacts on pH- and thermo-responsiveness of tertiary amine functionalized polypeptides
Xiao, Chunsheng,Cheng, Yilong,Zhang, Yu,Ding, Jianxun,He, Chaoliang,Zhuang, Xiuli,Chen, Xuesi
, p. 671 - 679 (2014/02/14)
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
Synthesis and structure-activity relationships of juvenoids derived from 2-(4-hydroxybenzyl)cycloalkan-1-ones
Rejzek,Wimmer,Saman,Ricankova,Nemec
, p. 1241 - 1255 (2007/10/02)
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.
