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【结 构 式】

【药物名称】Finrozole, MPV-2213ad

【化学名称】(±)-(R*,S*)-4-[3-(4-Fluorophenyl)-2-hydroxy-1-(1,2,4-triazol-1-yl)propyl]benzonitrile

【CA登记号】160146-17-8, 160146-16-7 (racemic (R*,R*)-isomer), 204714-56-7 (undefined stereochem.)

【 分 子 式 】C18H15FN4O

【 分 子 量 】322.34485

【开发单位】Orion Corp. (Originator), Hormos (Licensee)

【药理作用】Benign Prostatic Hyperplasia Therapy, Oncolytic Drugs, RENAL-UROLOGIC DRUGS, Aromatase Inhibitors

合成路线1

MPV-2213ad was synthesized by condensation of 4-(1,2,4-triazol-1-ylmethyl)benzonitrile (I) with 2-(4-fluorophenyl)acetaldehyde (II) by means of butyllithium in THF. The two diastereomeric racemates are separated by flash chromatography.

1 Silvestre, J.S.; Castañer, J.; Sorbera, L.A.; MPV-2213ad. Drugs Fut 1998, 23, 10, 1071-1074.
2 Karjalainen, A.J.; Sodervall, M.-L.; Kalapudas, A.M.; Pelkonen, R.O.; Laine, A.M.; Lammintausta, R.A.S.; Salonen, J.S. (Orion Corporation); Cyanobenzyl heterocyclic aromatase-inhibiting cpds.. GB 2273704; JP 1996504424; US 5703109; US 5962495; WO 9413645 .
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) 14202 4-(1H-1,2,4-Triazol-1-ylmethyl)benzonitrile C10H8N4 详情 详情
(II) 17588 2-(4-fluorophenyl)acetaldehyde C8H7FO 详情 详情
Extended Information