76101-29-6Relevant articles and documents
COMPOUNDS FOR TREATING CANCER
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Paragraph 0241, (2020/11/23)
Provided herein are prodrugs of 5-fluorodeoxyuridine monophosphate compounds, compositions thereof, methods of their preparation, and their use in treating cancers. In another aspect, provided herein is a pharmaceutical composition comprising any compound disclosed herein, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier, diluent, and excipient.
Synthesis and enzymatic evaluation of phosphoramidon and its β anomer: Anomerization of α-L-rhamnose triacetate upon phosphitylation
Sun, Qi,Yang, Qingkun,Gong, Shanshan,Fu, Quanlei,Xiao, Qiang
, p. 6778 - 6787 (2013/10/22)
A novel and efficient strategy for the synthesis of phosphoramidon and its β anomer has been developed by manipulating the anomerization of α-l-rhamnose triacetate upon phosphitylation. The experimental results suggest that proton transfer, bond rotation, and N atom are the key factors for the anomerization. The determined Ki and Kd values establish that phosphoramidon prepared by this method possesses excellent biological activity, and indicate that the contacts of rhamnose moiety with the enzyme have limited contribution to the binding.
PROCESS FOR PREPARING PHOSPHORYLATED AMINO ACIDS
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Page/Page column 79; 80, (2013/03/26)
The present invention provides a short, safe, inexpensive, commercially scalable process for preparing a phosphorylated amino acid of Formula I, which can be performed in one pot without isolating any synthetic intermediates.
PROCESS FOR PREPARING PHOSPHORYLATED AMINO ACIDS
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Page/Page column 72, (2013/03/26)
The present invention provides a short, safe, inexpensive, commercially scalable process for preparing a phosphorylated amino acid of Formula I, which can be performed in one pot without isolating any synthetic intermediates.
A P(V)-N activation strategy for the synthesis of nucleoside polyphosphates
Sun, Qi,Gong, Shanshan,Sun, Jian,Liu, Si,Xiao, Qiang,Pu, Shouzhi
, p. 8417 - 8426 (2013/09/24)
A general and high-yielding synthesis of nucleoside 5′-triphosphates (NTPs) and nucleoside 5′-diphosphates (NDPs) from protected nucleoside 5′-phosphoropiperidates promoted by 4,5-dicyanoimidazole (DCI) has been developed. 31P NMR tracing experiments showed that the sequential deprotection and coupling reactions were exceptionally clean. The phosphoropiperidate exhibited superior reactivity to the conventional phosphoromorpholidate toward DCI-promoted NTP/NDP synthesis. The experimental results suggested that the mechanism of DCI activation could be distinctive for NTP and NDP synthesis, depending on the different nucleophilicity of pyrophosphate and phosphate.
A general preparation of protected phosphoamino acids
Petrillo, Daniel E.,Mowrey, Dale R.,Allwein, Shawn P.,Bakale, Roger P.
supporting information; experimental part, p. 1206 - 1209 (2012/05/04)
Fmoc-O-benzyl-l-phosphoserine is an important building block in the synthesis of Forigerimod, a phosphopeptide being investigated for Systemic Lupus Erythematosus (SLE). An efficient one-pot process was developed using inexpensive, readily available starting materials. This general procedure was used to prepare a variety of protected phosphoamino acids.
BODP - A versatile reagent for phospholipid synthesis
Zaffalon, Pierre-Leonard,Zumbuehl, Andreas
experimental part, p. 778 - 782 (2011/04/22)
Benzyloxydichlorophosphine (BODP) has been found to be a convenient reagent for the synthesis of phospholipids. A series of artificial ether and ester phospholipids have been prepared in good to high yields. Georg Thieme Verlag Stuttgart New York.
The synthesis of an amine-bearing polymerizable phospholipid
Zaffalon, Pierre-Leonard,Stalder, Etienne,Fedotenko, Illya A.,Favarger, France,Zumbuehl, Andreas
supporting information; experimental part, p. 4215 - 4217 (2011/09/19)
Exchange of the natural glycerol phospholipid backbone with an artificial 1,3-diaminopropanol backbone led to the first synthetic 1,3-diaminophospholipid. The amines in the polar head group region were reacted to acrylamides giving a UV polymerizable phospholipid. Preliminary experiments demonstrate that formulated vesicles can be polymerized into large aggregates of vesicles.
New approach to the synthesis of phosphorodichloridites, phosphorochloridites, and trialkyl phosphites
Majewski, Piotr
experimental part, p. 942 - 955 (2010/01/17)
Different trivalent organophosphorus esters such as phosphorodichloridites, phosphorochloridites, and mixed trialkyl phosphites have been easily synthesized in good yields using a HCl-catalyzed reaction of the corresponding chlorophosphine and alkoxytrimethylsilane by mutual exchange of the alkoxy and chlorine ligand pIIICl/ROSiR′3; exchange reaction). Chemoselectivity of the exchange reaction with primary and secondary alkoxytrimethylsilanes, as well as with alkoxytrimethylsilanes and thioalkoxytrimethylsilanes, respectively, has also been examined. It has been also found that the substitution reaction of chlorophosphines with secondary amine occurs more rapidly than the exchange reaction with ROSiR′ 3.
Synthesis of cyclophospho-glucoses and glucitols
Amigues,Greenberg,Ju,Chen,Migaud
, p. 10042 - 10053 (2008/02/13)
The syntheses of cyclophosphodiesters of 5-C-(hydroxymethyl)-hexoses and hexitols and of 6-C-(hydroxymethyl)-hexoses are reported, along with that of 6-deoxy-gluco-heptose 7-phosphate. These compounds proved to be reasonable substrate mimics and show inhibitory activity against human d-myo-inositol 3-phosphate synthase.
