42268-68-8Relevant articles and documents
Chemoproteomics-Enabled De Novo Discovery of Photoswitchable Carboxylesterase Inhibitors for Optically Controlled Drug Metabolism
Dwyer, Brendan G.,Wang, Chao,Abegg, Daniel,Racioppo, Brittney,Qiu, Nan,Zhao, Zhensheng,Pechalrieu, Dany,Shuster, Anton,Hoch, Dominic G.,Adibekian, Alexander
, p. 3071 - 3079 (2021)
Herein, we report arylazopyrazole ureas and sulfones as a novel class of photoswitchable serine hydrolase inhibitors and present a chemoproteomic platform for rapid discovery of optically controlled serine hydrolase targets in complex proteomes. Specifica
West request acid bei geleg sandbank and intermediate preparation method
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Paragraph 0077-0081, (2019/02/26)
The invention relates to a preparation method of besigliptin and its intermediate, and concretely relates to a preparation method of an azadicyclic compound besigliptin and its key intermediate. The preparation method comprises the following steps: carrying out step a, step b and step c to prepare the key intermediate compound of formula VII, carryin gout isomer resolution and protective group removal on the compound of formula VII to obtain a compound of formula XV, coupling the compound of formula XV with the compound of formula XIII, and salifying to form a target compound I. The preparation method has the advantages of substantial reduction of the production cost, simple production flow, yield increase, and suitableness for industrial production.
A two-directional strategy for the diversity-oriented synthesis of macrocyclic scaffolds
O'Connell, Kieron M. G.,Beckmann, Henning S. G.,Laraia, Luca,Horsley, Helen T.,Bender, Andreas,Venkitaraman, Ashok R.,Spring, David R.
, p. 7545 - 7551 (2012/10/29)
Macrocyclic compounds represent a structural class with exceptional potential for biological activity; however, they have historically been underrepresented in screening collections and synthetic libraries. In this article we report the development of a highly step-efficient strategy for the diversity-oriented synthesis of complex macrocyclic architectures, using a modular approach based on the two-directional synthesis of bifunctional linear precursors and their subsequent combination in a two-directional macrocyclisation process. In this proof of principle study, the synthesis of 14 such compounds was achieved. Cheminformatic analysis of the compounds produced suggests that they reside in biologically relevant regions of chemical space and the compounds were screened for activity against two cancer cell lines.