146578-12-3Relevant articles and documents
Phosphoramidite nucleoside derivative as well as synthesis method, application and kit thereof
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, (2022/04/15)
The invention discloses a phosphoramidite nucleoside derivative as well as a synthesis method, application and a kit thereof, and belongs to the field of oligonucleotides. The synthesis method comprises the following steps: protecting hydroxyl of an initiator, protecting N6-site amino on a basic group, and then removing protection of 3 'and 5' hydroxyl to obtain a first intermediate; protecting 5'and 3 'hydroxyl groups of the first intermediate to obtain a second intermediate; removing a protecting group of 5'hydroxyl of the second intermediate, and protecting the 5 'hydroxyl through methoxy isopropyl to obtain a third intermediate; sequentially removing protecting groups of 3'hydroxyl and N6 amino on the basic group in the third intermediate to obtain a fourth intermediate; and carrying out imidization protection on an N6-site amino group on a basic group of the fourth intermediate, and carrying out phosphoramidation protection on a 3 '-hydroxyl group. The method has the advantages of being convenient to implement, economical and capable of achieving large-scale production.
CYCLIC DINUCLEOTIDES AS STING AGONISTS
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Page/Page column 191-192, (2019/07/19)
Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein B2,X2, R2a, R2b, R2c, Z-M-Y, Y1-M1Z1, B1, X1, R1a, R1b, R1c are as defined herein.
Design, efficient synthesis, and anti-HIV activity of 4′-C-cyano- and 4′-C-ethynyl-2′-deoxy purine nucleosides
Kohgo, Satoru,Yamada, Kohei,Kitano, Kenji,Iwai, Yuko,Sakata, Shinji,Ashida, Noriyuki,Hayakawa, Hiroyuki,Nameki, Daisuke,Kodama, Eiichi,Matsuoka, Masao,Mitsuya, Hiroaki,Ohrui, Hiroshi
, p. 671 - 690 (2007/10/03)
Some 4′-C-ethynyl-2′-deoxy purine nucleosides showed the most potent anti-HIV activity among the series of 4′-C-substituted 2′-deoxynucleosides whose 4′-C-substituents were methyl, ethyl, ethynyl and so on. Our hypothesis is that the smaller the substitue