76-39-1Relevant articles and documents
Chachaty,Forchioni
, p. 1079 (1968)
Green synthesis method for one-pot process preparation of AMP-95
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Paragraph 0033; 0035; 0037; 0039; 0041; 0043; 0045; 0046, (2018/07/07)
The invention discloses a green synthesis method for the one-pot process preparation of AMP-95. The method comprises the following steps: S1, preparing 2-nitropropane from acetone, hydrogen peroxide and ammonia in an alcohol solution under the catalysis of a catalyst; S2, directly reacting a reaction solution obtained in step S1 with formaldehyde or paraformaldehyde under an alkaline condition without purifying in order to generate 2-nitro-2-methyl-1-propanol; and S3, directly hydrogenating the reaction product obtained in step S2 without purifying to obtain the product 2-amino-2-methy-1-propanol (AMP-95), and rectifying the product to make the purity reach 99.5% or more. The method has the advantages of cheap and easily available raw materials, simple reaction steps, small pollution to the environment, low cost, high yield, easiness in purification of the product, and suitableness for industrial production.
Synthesis and Evaluation of a Library of Trifunctional Scaffold-Derived Compounds as Modulators of the Insulin Receptor
Fabre, Benjamin,Pícha, Jan,Vaněk, Václav,Selicharová, Irena,Chrudinová, Martina,Collinsová, Michaela,?áková, Lenka,Budě?ínsky, Milo?,Jirá?ek, Ji?í
supporting information, p. 710 - 722 (2016/12/22)
We designed a combinatorial library of trifunctional scaffold-derived compounds, which were derivatized with 30 different in-house-made azides. The compounds were proposed to mimic insulin receptor (IR)-binding epitopes in the insulin molecule and bind to and activate this receptor. This work has enabled us to test our synthetic and biological methodology and to prove its robustness and reliability for the solid-phase synthesis and testing of combinatorial libraries of the trifunctional scaffold-derived compounds. Our effort resulted in the discovery of two compounds, which were able to weakly induce the autophosphorylation of IR and weakly bind to this receptor at a 0.1 mM concentration. Despite these modest biological results, which well document the well-known difficulty in modulating protein-protein interactions, this study represents a unique example of targeting the IR with a set of nonpeptide compounds that were specifically designed and synthesized for this purpose. We believe that this work can open new perspectives for the development of next-generation insulin mimetics based on the scaffold structure.
