Iproxifene, Miproxifene phosphate, TAT-59-药物合成数据库

【药物名称】Iproxifene, Miproxifene phosphate, TAT-59

化学结构式(Chemical Structure):

参考文献No.	7397
标题:	1,1,2-Triaryl-1-butene derivs.
作者:	Asao, T.; Takeda, S.; Sugimoto, Y.; Toko, T.; Yamada, Y.; Ogawa, K.; Unemi, N. (Taiho Pharmaceutical Co., Ltd.)
来源:	AU 8775199; JP 1988503618; US 4897503; WO 8707609

合成路线图解说明: The Grignard condensation of 4'-[2-(dimethylamino)ethoxy]-2-(4-isopropylphenyl)butyrophenone (I) with 4-(2-tetrahydropyranyloxy)phenylmagnesium bromide (II) in refluxing THF gives the triphenylbutanol derivative (III). The dehydration and deprotection of (III) by means of HCl in ethanol yields (E)-4-[1-[4-[2-(dimethylamino)ethoxy)phenyl]-2-(4-isopropylphenyl)-1-butenyl]phenol (IV), which is finally esterified with POCl3 in pyridine and hydrolyzed with NaHCO3 in ice water followed by acidification with concentrated HCl.

参考文献No.	135682
标题:	TAT-59
作者:	Hoshi, A.
来源:	Drugs Fut 1991,16(3),217

合成路线图解说明: The Grignard condensation of 4'-[2-(dimethylamino)ethoxy]-2-(4-isopropylphenyl)butyrophenone (I) with 4-(2-tetrahydropyranyloxy)phenylmagnesium bromide (II) in refluxing THF gives the triphenylbutanol derivative (III). The dehydration and deprotection of (III) by means of HCl in ethanol yields (E)-4-[1-[4-[2-(dimethylamino)ethoxy)phenyl]-2-(4-isopropylphenyl)-1-butenyl]phenol (IV), which is finally esterified with POCl3 in pyridine and hydrolyzed with NaHCO3 in ice water followed by acidification with concentrated HCl.