The invention relates to the use of an amine masked moiety in a method of enzymatic nucleic acid synthesis. The invention also relates to said amine masked moieties per se and a process for preparing nucleotide triphosphates comprising said amine masked moieties.

It is provided i) an amorphous carbohydrate with improved chemical stability and/or physical features, ii) a method for producing an amorphous carbohydrate with improved chemical stability and/or physical features, and iii) a method for improving the chemical stability and/or the physical features of an amorphous carbohydrate.

It is provided i) an amorphous carbohydrate with improved chemical stability and/or physical features, ii) a method for producing an amorphous carbohydrate with improved chemical stability and/or physical features, and iii) a method for improving the chemical stability and/or the physical features of an amorphous carbohydrate.

In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

The present application provides a small-molecule compound, represented by general Formula (I), having A.sub.2A adenosine receptor antagonistic activity and a pharmaceutical composition containing same. The compound and composition can be used as A.sub.2A adenosine receptor antagonistic agents.

##STR00001##

A first derivative of a fullerene is covalently bonded to an adenosine phosphate such as adenosine triphosphate, adenosine diphosphate, adenosine monophosphate, or cyclic adenosine monophosphate. A second fullerene is covalently bonded to a second type of functional group including amines of arginine and lysine. The second fullerene is then van-der-Waals bonded to the first fullerene, to form a biaxially pivoting fullerene molecular composition. This composition can be treated to intercalate and carry a drug or an antibody for later release by directed irradiation. The injected composition with optional drug carrier is electrodynamically activated by irradiation of the injected target organ or tissues by the application of, for example, radio frequency (RF) energy to release the drug and lyse the targeted cells.

The invention relates to a method for preparing nicotinamide mononucleotide by using nicotinamide as a raw material, which comprises: in acetonitrile, dichloromethane, 1,2-dichloroethane or liquid sulfur dioxide as a solvent, allowing nicotinamide and tetraacetyl ribose to react as catalyzed by trimethylsilyl trifluoromethanesulfonate or tin tetrachloride, adjusting a pH value thereof to 3-5, adding a sodium methoxide solution thereto to react at −15° C. to 5° C., adjusting a pH value thereof to 3-5, and subjecting the reaction mixture to microfiltration and nanofiltration using a membrane concentrator, thereby obtain a nicotinamide ribose solution; allowing the nicotinamide ribose solution to react as catalyzed by nicotinamide ribokinase in the presence of Mg ions, ATP and a buffer, thereby obtaining nicotinamide mononucleotide. The method of the invention omits the step of refining nicotinamide ribose, and thus has simpler process, lower cost and less time consumption, and has the advantages of faster reaction speed and lower enzyme consumption compared with the enzyme catalytic process directly using refined nicotinamide ribose solid.

Methods of preparing nicotinamide riboside and derivatives thereof. In an aspect, the invention relates to a method of preparing a compound of formula (I) ##STR00001##
wherein
n is 0 or 1;
m is 0 or 1;
Y is O or S; R.sub.1 is selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted primary or secondary amino, and substituted or unsubstituted azido; R.sub.2-R.sub.5, which may be the same or different, are each independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, and substituted or unsubstituted aryl; and X.sup.− is an anion, selected from an anion of a substituted or unsubstituted carboxylic acid, a halide, a substituted or unsubstituted sulfonate, a substituted or unsubstituted phosphate, a substituted or unsubstituted sulfate, a substituted or unsubstituted carbonate, and a substituted or unsubstituted carbamate.

Methods of preparing nicotinamide riboside and derivatives thereof. In an aspect, the invention relates to a method of preparing a compound of formula (I) ##STR00001##
wherein
n is 0 or 1;
m is 0 or 1;
Y is O or S; R.sub.1 is selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted primary or secondary amino, and substituted or unsubstituted azido; R.sub.2-R.sub.5, which may be the same or different, are each independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, and substituted or unsubstituted aryl; and X.sup.− is an anion, selected from an anion of a substituted or unsubstituted carboxylic acid, a halide, a substituted or unsubstituted sulfonate, a substituted or unsubstituted phosphate, a substituted or unsubstituted sulfate, a substituted or unsubstituted carbonate, and a substituted or unsubstituted carbamate.