- Preparation method of primaquine phosphate
-
The invention discloses a preparation method of primaquine phosphate, which is characterized by comprising the following steps of: adding a secondary condensate, ethanol and hydrazine hydrate into a reaction container, introducing nitrogen for protection, stirring in a dark place, heating to 78-80 DEG C, carrying out reflux reaction until the reaction is complete, evaporating ethanol under normal pressure until the internal temperature is increased to 92-95 DEG C, adding water, stirring, heating to 58-62 DEG C to enable no solid to suspend, cooling to 40-50 DEG C, dropwise adding a sodium hydroxide solution with the mass concentration of 25-30% while stirring to enable the pH to be 13-14, stirring, adding methylbenzene, stirring, standing for layering, adding water into an organic phase for washing, then decolorizing with activated carbon, filtering and concentrating to obtain free primaquine oil, and adding dichloroethane for crystallization to obtain free primaquine. By adjusting process parameters (such as reaction temperature, time, light shielding, nitrogen protection and charging sequence) of each step, a dichloroethane crystallization process of free primaquine is added, the purity of a finished product is greater than 99.5%, the content of a single impurity is less than 0.2%, and the yield is high.
- -
-
Paragraph 0055-0072
(2021/08/14)
-
- Synthesis of primaquine glyco-conjugates as potential tissue schizontocidal antimalarial agents
-
Primaquine (PQ) is the only drug used to prevent relapse of malaria due to P. vivax and P. ovale, by eradicating the dormant liver form of the parasite (hypnozoites). The side-effects associated with PQ limits is uses in treatment of malaria. To overcome the premature oxidative deamination and to increase the life span of drug in the biological system, the novel glyco-conjugates of PQ were synthesized by coupling of primaquine with hexoses in phosphate buffer. The saccharide part of the hybrid molecules thought to direct the drug to the liver, where hypnozoites resides. All the synthesized compounds were fully characterized and evaluated for their radical curative activities. The three compounds viz glucoside (15a), galactoside (15b) and mannoside (15c) with high activity were tested for their activity in rhesus monkeys where the most active compound 15b showed twofold activity (100% radical curative activity at 1.92?mmol/kg) than the standard drug PQ diphosphate (3.861?mmol/kg). It is proposed that results from these studies may be advantageous to develop a new potent tissue schizonticide antimalarial compound.
- Azad, Chandra S.,Saxena, Mridula,Siddiqui, Arif J.,Bhardwaj, Jyoti,Puri, Sunil K.,Dutta, Guru P.,Anand, Nitya,Saxena, Anil K.
-
p. 254 - 261
(2017/07/13)
-
