The disclosure includes zinc prodrugs for targeted delivery of therapeutic, diagnostic or imaging agents to β-cells and methods of use therefor. The disclosure also includes targeted delivery of small molecules to β-cells that stabilize and activate CRISP
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(2018/11/22)
Method of synthesizing [...]
PURPOSE: A method for synthesizing sivelestat is provided to perform reaction without separation of intermediates and to improve yield and productivity. CONSTITUTION: A method for synthesizing sivelestat comprises the steps of: (i) reacting 4-pivaloyloxy benzenesulfonate salts with halogenating agents to obtain 4-(halosulfonyl)phenyl pivalate; (ii) reacting isatoic anhydride with benzyl glycinate to obtain benzyl 2-(2-aminobenzamido)acetate; (iii) reacting the products obtained from steps (i) and (ii) to obtain 4-(N-(2-(2-(benzyloxy)-2-oxoethylcarbamoyl)phenyl)sulfamoyl)phenyl pivalate; and (iv) performing debenzylation of the product of step (iii) to obtain sivelestat.
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(2016/12/16)
Efficient synthesis of sivelestat sodium hydrate
An efficient and scaleable synthesis of sivelestat sodium hydrate has been developed. Copyright Taylor & Francis Group, LLC.
Bijukumar,Maloyesh,Sampat,Bhirud,Rajendra
p. 1718 - 1724
(2008/09/20)
Non-peptidic inhibitors of human neutrophil elastase: The design and synthesis of sulfonanilide-containing inhibitors
A novel series of pivaloyloxy benzene derivatives has been identified as potent and selective human neutrophil elastase (HNE) inhibitors. Convergent syntheses were developed in order to identify the inhibitors which are intravenously effective in an animal model. A compound of particular interest is the sulfonanilide-containing analogues. Structure-activity relationships are discussed. Structural requirements for metabolic stabilization are also discussed.