Minodronic Acid

한글명:Minodronic Acid

카스 번호155648-60-5

상품명:Minodronic Acid

CBNumberCB82521286

분자식C9H14N2O8P2

포뮬러 무게340.163582

MOL 파일155648-60-5.mol

화학적 성질

저장 조건	2-8°C
수용성	물에 불용성
물리적 상태	powder to crystal
색상	White to Light yellow to Light red
InChI	InChI=1S/C9H12N2O7P2.H2O/c12-9(19(13,14)15,20(16,17)18)5-7-6-10-8-3-1-2-4-11(7)8;/h1-4,6,12H,5H2,(H2,13,14,15)(H2,16,17,18);1H2
InChIKey	GPAPAOGRNKUFGH-UHFFFAOYSA-N
SMILES	C(P(O)(O)=O)(O)(P(O)(O)=O)CC1N2C(=NC=1)C=CC=C2.[H]O[H]

위험 및 안전 성명

유엔번호(UN No.)	2811
RTECS 번호	SZ8562470
HS 번호	2933.99.8290
위험 등급	6.1
포장분류	III

그림문자(GHS)

Minodronic Acid 화학적 특성, 용도, 생산

Mechanism of action
Third-generation bisphosphonates, including minodronic acid hydrate, contain an amino group in the imidazole ring and are even more powerful inhibitors of bone resorption. With regard to inhibition of bone resorption, minodronic acid hydrate is 1000 times more effective than etidronate and 10–100 times more effective than alendronic acid. Following administration, minodronic acid hydrate specifically accumulates in the bone. It is then separated from the bone by acid released by osteoclasts during the bone resorption process and selectively taken up by osteoclasts. Conventional bisphosphonates were believed to inhibit bone resorption through the induction of osteoclast apoptosis after being taken up by these cells[1].
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.

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