Minodronic Acid Chemical Properties

storage temp. 

2-8°C

Water Solubility 

Insoluble in water

form 

powder to crystal

color 

White to Light yellow to Light red

Safety Information

RIDADR 

2811

RTECS 

SZ8562470

HS Code 

2933.99.8290

HazardClass 

6.1

PackingGroup 

III

Minodronic Acid Usage And Synthesis

Clinical Use

The bone resorption inhibitor minodronic acid hydrate was approved and introduced last year in Japan, bringing the total number of bis-phosphonates marketed for this indication to seven. There are an estimated 10 million current and potential osteoporosis sufferers in Japan, a number that is expected to continue growing due to the country’s aging population. Minodronic acid is the first drug to show a significant effect in preventing bone fractures as compared to placebo in a Japanese patient population. Minodronic acid was co-developed by Astellas and Ono, who are marketing the drug as Bonoteo and Recalbon, respectively.

Synthesis

Several syntheses of minodronic acid have been reported,a scalable preparation is described in the scheme. Commercially available acid chloride 71 was first reduced with lithium tritertbutoxy aluminum hydride to the aldehyde 72 at 80??C in 61% yield. Next, reaction of aldehyde 72 with TMSCl and triethylamine generated the corresponding silyl enol ether, which was then treated with bromine to give a-bromoaldehyde 73 in 62% yield. Condensation with 2-amino pyridine furnished imidazopyridine 74, which was hydrolyzed with HCl to acid 75 in 58% yield. Reaction with H3PO3 at 120??C to provide minodronic acid hydrate (XII) in 53% yield.

Minodronic Acid(155648-60-5)Related Product Information

• MINODRONATE
• Ipriflavone