|
【结 构 式】 
|
【药物名称】TZA-2237 【化学名称】7alpha-Mercapto-17-oxa-17a-homoandrosta-1,4-diene-3,17a-dione 【CA登记号】159822-03-4 【 分 子 式 】C19H24O3S 【 分 子 量 】332.46533 |
【开发单位】Teikoku Hormone (Originator) 【药理作用】Benign Prostatic Hyperplasia Therapy, RENAL-UROLOGIC DRUGS, Aromatase Inhibitors |
合成路线1
Treatment of D-homo-17-oxaandrosta-1,4,6-triene-3,17a-dione (I) with refluxing thioacetic acid (II) yields either 7-alpha-(acetylthio) derivative (III) or 1alpha,7alpha-bis(acetylthio) derivative (IV). The desired product can then be obtained either by treatment of (III) with NaOH in THF or by reaction of (IV) with sodium methylate in methanol.
| 【1】 Koizumi, N.; Takegawa, S.; Iwashita, S.; Kawachi, T.; Inoue, F.; Honma, S.; Takahashi, H.; Mieda, M.; Ueda, K.; Shibata, K. (Teikoku Hormone Manufacturing Co., Ltd.); Novel 7-substd. oxa- or azasteroid cpd.. EP 0663402; JP 1994508897; US 5539127; WO 9407908 . |
| 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) | 46697 | (4aS,4bR,10aS,10bS,12aS)-10a,12a-dimethyl-3,4,4a,10a,10b,11,12,12a-octahydro-1H-naphtho[2,1-f]isochromene-1,8(4bH)-dione | C19H22O3 | 详情 | 详情 | |
| (II) | 12893 | Ethanethioic S-acid | C2H4OS | 详情 | 详情 | |
| (III) | 46698 | S-[(4aS,4bR,5R,10aR,10bS,12aS)-10a,12a-dimethyl-1,8-dioxo-3,4,4a,4b,5,6,8,10a,10b,11,12,12a-dodecahydro-1H-naphtho[2,1-f]isochromen-5-yl] ethanethioate | C21H26O4S | 详情 | 详情 | |
| (IV) | 46699 | S-[(4aS,4bS,5R,10S,10aR,10bS,12aS)-10-(acetylsulfanyl)-10a,12a-dimethyl-1,8-dioxo-3,4,4a,4b,5,6,8,9,10,10a,10b,11,12,12a-tetradecahydro-1H-naphtho[2,1-f]isochromen-5-yl] ethanethioate | C23H30O5S2 | 详情 | 详情 |
Extended Information