Mofezolac, N-22, Disopain, -Drug Synthesis Database

【结构式】

【药物名称】Mofezolac, N-22, Disopain

【化学名称】3,4-Bis(4-methoxyphenyl)-5-isoxazoleacetic acid
　　　　　　3,4-Di-(p-methoxyphenyl)isoxazole-5-acetic acid

【CA登记号】78967-07-4

【分子式】C₁₉H₁₇NO₅

【分子量】339.35104

【开发单位】Mitsubishi Pharma (Originator), Taiho (Originator)

【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Non-Opioid Analgesics, Non-Steroidal Antiinflammatory Drugs

合成路线1

The reaction of desoxyanisoin (I) with hydroxylamine in methanol gives the corresponding oxime (I), which is cyclized with ethyl acetate (III) by means of n-butyllithium in THF yielding 3,4-di(4-methoxyphenyl)-5-methylisoxazole (IV). Finally, this compound is condensed with CO2 by means of n-butyllithium in THF.

参考文献中间体

【1】 Micetich, R.G.; Shaw, C.-C.; Rastogi, R.B. (CDC Life Sciences Inc.); 3,4-Diaryl-5-acetic acid cpds., process for prepar. EP 0026928; US 4327222 .
【2】 Prous, J.; Castaner, J.; N-22. Drugs Fut 1988, 13, 12, 1050.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	22991	1,2-bis(4-methoxyphenyl)-1-ethanone	120-44-5	C₁₆H₁₆O₃	详情	详情
(II)	22992	1,2-bis(4-methoxyphenyl)-1-ethanone oxime		C₁₆H₁₇NO₃	详情	详情
(III)	17941	3-Trimethylsilylpropargyl alcohol; 3-(trimethylsilyl)-2-propyn-1-ol	5272-36-6	C₆H₁₂OSi	详情	详情
(IV)	22994	4-[3-(4-methoxyphenyl)-5-methyl-4-isoxazolyl]phenyl methyl ether; 3,4-bis(4-methoxyphenyl)-5-methylisoxazole		C₁₈H₁₇NO₃	详情	详情

Extended Information