- Synthesis method of isocytosine
-
The invention provides a synthesis method of isocytosine. The synthesis method comprises the following steps: step a), synthesizing sodium hydroxyethyl acrylate: after mixing ethyl formate and a catalyst according a certain mole ratio under the condition that the temperature is -5 DEG C to 0 DEG C, heating and reflowing; slowly dropwise adding ethyl acetate to obtain the sodium hydroxyethyl acrylate; step b), synthesizing the isocytosine: adding guanidine hydrochloride for synthesizing the isocytosine into the prepared sodium hydroxyethyl acrylate; after heating and reflowing, evaporating to dry a residual solvent; adding water into a concentrated object obtained by evaporation and dissolving; then regulating the pH (Potential of Hydrogen) to be neutral with acid; then evaporating the obtained solution to be dry and removing unreacted raw materials to obtain an isocytosine pure product, and drying. According to the method provided by the invention, the raw materials do not contain chemicals which easily cause toxin, have a wide source and do not cause damages to human bodies and environments; furthermore, reactants are mixed under the condition that the temperature is -5 DEG C to 0 DEG C in a synthesis process of the sodium hydroxyethyl acrylate, the generation of byproducts can be reduced and the yield of the isocytosine is improved.
- -
-
Paragraph 0030; 0031; 0032; 0040; 0041; 0042
(2018/03/28)
-
- ANTIVIRAL AGENT
-
The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)
- -
-
-
- Development of an efficient and straightforward methodology toward the synthesis of molecularly diverse 2,6-disubstituted 3,4-dihydropyrimidin-4(3H)-ones
-
A simple and efficient methodology toward the synthesis of highly molecularly diverse 2,6-disubstituted 3,4-dihydropyrimidin-4(3H)-ones of type 3 has been developed. The methodology is based on a selective O-alkylation reaction with i-PrOH under Mitsunobu conditions followed by a nucleophilic heteroaromatic ipso-substitution of sulfones 20 and subsequent acidic hydrolysis of the isopropoxy group.
- Font, David,Heras, Montserrat,Villalgordo, Jose? M.
-
p. 1833 - 1842
(2007/10/03)
-
- PIPERAZINE SUBSTITUTED PYRIMIDINE DERIVATIVES AND PHYSIOLOGICALLY TOLERATED SALTS THEREOF
-
Pyrimidine derivatives of the formula I I in which R1, R2, R3, R4 and R5 have the indicated meanings, the salts thereof, and a process for the preparation thereof are described. Because of their sorbitol-accumulating activity, they are suitable as a tool in a pharmacological screening model for aldose reductase inhibitors
- -
-
-
- A Facile Method for the Preparation of 2-Substituted Pyrimidin-4(3H)-ones by a Retro-Diels-Alder Reaction
-
diexo-3-Aza-4-oxotricyclo2.5>non-7-ene (1) reacted with carboximidic esters by ring expansion to yield tricyclic 5,6-dihydropyrimidin-4(3H)-ones 3; when the latter were refluxed in chlorobenzene solution, cyclopentadiene split off to gi
- Stajer, Geza,Szabo, Angela E.,Bernath, Gabor,Sohar, Pal
-
p. 290 - 292
(2007/10/02)
-
