108296-16-8Relevant academic research and scientific papers
GalNAc CLUSTER PHOSPHORAMIDITE
-
, (2017/06/12)
The invention comprises Gal NAc phosphoramidite derivatives of the formula (I), wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/ or optical isomers thereof. The invention further comprises a process for the preparation of the Gal NAc phosphoramidite derivatives of the formula (I) and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.
Triphenylphosphinecarboxamide: An effective reagent for the reduction of azides and its application to nucleic acid detection
Saneyoshi, Hisao,Ochikubo, Tatsuya,Mashimo, Takushi,Hatano, Ken,Ito, Yoshihiro,Abe, Hiroshi
, p. 30 - 33 (2014/01/23)
A series of triphenylphosphinecarboxamide (TPPc) derivatives were designed and synthesized as alternative reagents to triphenylphosphine for the facile reduction of azides. The TPPc derivatives performed as efficient reducing agents for the synthesis of primary amines without the need for an additional hydrolysis procedure. The TPPc derivatives were also applied to nucleic acid sensing using a RhAz-oligonucleotide conjugate in a DNA-templated fluorogenic reaction.
Structure-Activity Relationships among Di- and Tetramine Disulfides Related to Benextramine
Alvarez, M.,Granados, R.,Mauleon, D.,Rosell, G.,Salas, M.,et al.
, p. 1186 - 1193 (2007/10/02)
The synthesis and irreversible α-blocking activity in the rat vas deferens of a series of tetra- and diamine disulfides 2-38, structural analogues of benextramine (BHC), are described. All compounds containing a central cystamine moiety displayed an irreversible α-adrenergic blockade at concentrations ranging from 10-4 to 6*10-6 M. Potency was increased in cystamines N,N'-disubstituted with 6-aminohexyl groups, especially when the outer nitrogen atoms bear arylalkyl substituents or are enclosed in a ring. However, N,N,N',N'-tetrasubstituted cystamines were poor blockers. Structural specificity in the outer portion of the tetramine disulfide is low, since many types of substituents gave rise to potent α-blockers. Even replacement of the outer amines with nonbasic ethers or amides was observed to maintain irreversible α-blockade.
