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【结 构 式】 
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【分子编号】45443 【品名】Benzofuran-2-carbaldehyde; 1-benzofuran-2-carbaldehyde 【CA登记号】4265-16-1 |
【 分 子 式 】C9H6O2 【 分 子 量 】146.14544 【元素组成】C 73.97% H 4.14% O 21.9% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(II)Compound (I) (intermediate no. (VIII) in scheme no. 19918301a) is a key intermediate in the synthesis of indinavir. For the synthesis of the product 285239, (I) is coupled with benzofuran-2-carbaldehyde (II) via a reductive amination by means of NaBH(OAc)3 either in 1,2-dichloroethane/AcOH or in isopropyl acetate/AcOH.
| 【1】 McDaniel, S.L.; McDonough, C.; Dorsey, B.D.; et al.; Identification of MK-944a: A second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. J Med Chem 2000, 43, 18, 3386. |
| 【3】 Lin, J.H.; Chodakewitz, J.A.; Deutsch, P.J.; Vacca, J.P.; Yeh, K.C.; Ju, W.D. (Merck & Co., Inc.); Combination therapy for the treatment of AIDS. WO 9925352 . |
| 【2】 Hoerrner, R.S.; Volante, R.P.; Purick, R.M.; Askin, D.; Reider, P.; Varsolona, R.J. (Merck & Co., Inc.); Sulfate salt of an HIV protease inhibitor having an improved oral absorption and bioavailability. EP 0986554; JP 2000513747; US 6071916; WO 9854178 . |
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