84960-04-3

Upstream product

• 82410-30-8 N²-acetyl-9-<<1,3-bis(benzyloxy)-2-propoxy>methyl>guanine 
• 75-44-5 phosgene 
• 19962-37-9 N-(6-oxo-6,9-dihydro-1H-purin-2-yl)acetamide 
• 105-70-4 2-hydroxypropane-1,3-diyl diacetate 
• 3056-33-5 2,9-diacetylguanine 
• 73-40-5 2-amino-1,9-dihydro-6H-purin-6-one 

Downstream Products

• 82410-32-0 ganciclovir 

Relevant academic research and scientific papers

9-[(1,3-dihydroxy-2-propoxy)methyl]guanine: A new potent and selective antiherpes agent

The synthesis of a new acyclic analogue of deoxyguanosine, 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine (DHPG, 1) is described starting from epichlorohydrin via condensation of 2-O-(acetoxymethyl)-1,3-di-O-benzylglycerol (5) with N2,9-diacetylguanine (6). In vitro studies indicate that DHPG is a potent and broad-acting (herpes simplex virus types 1 and 2, cytomegalovirus, and Epstein-Barr virus) antiherpetic agent. In vivo studies indicate its lack of toxicity [LD50 (mice) = 1-2 g/kg, ip] and its superiority over acyclovir [oral ED50 = 7 (mg/kg)/day vs. 550 (mg/kg)/day in HSV-2 infected mice].

Preparation method and application of ganciclovir

The invention belongs to the field of medicine synthesis, and discloses a preparation method and application of ganciclovir. According to the preparation method, N-(6-carbonyl-6, 9-dihydro-1H-purine-2-yl) acetamide and 2-hydroxy-1, 3-propylene diacetate are subjected to condensation with chloroformyl chloride at the same time, an obtained intermediate is subjected to hydrolysis, and ganciclovir is obtained. The preparation method of ganciclovir can effectively improve the utilization rate of raw materials, reduce the use cost of the raw materials in the production process, shorten the process flow, and reduce the occurrence of side reactions and the use amount of solvents. The preparation method is suitable for preparing ganciclovir, and the prepared ganciclovir is used for preparing ganciclovir for injection.

A novel approach to the synthesis of the purine anti-viral agent gancyclovir

The aim of this research is to synthesize gancyclovir, a purine anti-viral drug in large scale via simple intermediates. Reaction of guanine 1 with acetic anhydride followed by the attachment of the 2-O-acetoxymethyl-1,3-di-O-benzyl glycerol 3 as a side chain, subsequently lead to the production of N2acetyl-9-(1,3dibenzyloxy-2-propoxymethyl)guanine 6 and N2, acetyl-9-(1,3-dihydroxy-2-propoxymethyl)guanine 7 and finally synthesizing gancyclovir 8. Among many pathways to the synthesis of purine derivatives, our four step procedure results in good yield and is proved to be an economic way of large scale synthesis.