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【结 构 式】

【药物名称】Talosalate, BA-760402

【化学名称】1,3-Dihydro-3-oxo-1-isobenzofuranyl 2-acetyloxybenzoate

【CA登记号】66898-60-0

【 分 子 式 】C17H12O6

【 分 子 量 】312.28159

【开发单位】Bagó(Originator)

【药理作用】Antiplatelet Therapy, Coagulation Disorders Therapy, HEMATOLOGIC DRUGS, Non-Steroidal Antiinflammatory Drugs

合成路线1

1) The reaction of 3-bromophthalide with 2-hydroxybenzoic acid (I), previously salified with triethylamine in refluxing acetone gives 1,3-dihydro-3-oxo-1-isobenzofuranyl 2-hydroxybenzoate (II). Compound (II) is acetylated with acetic anhydride, using sulfuric acid as catalizer.

1 (Laboratorios Bagó); Nouveaux esters de l'acide benzoique substitue. BE 0884978 .
2 Castaner, J.; Prous, J.; Talosalate. Drugs Fut 1986, 11, 5, 394.
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) 15240 2-Hydroxybenzoic acid; Salicylic acid 69-72-7 C7H6O3 详情 详情
(II) 24561 3-oxo-1,3-dihydro-2-benzofuran-1-yl salicylate C15H10O5 详情 详情
(IV) 24560 3-Bromophthalide; 3-Bromo-2-benzofuran-1(3H)-one 6940-49-4 C8H5BrO2 详情 详情

合成路线2

2) By condensation of an organic salt of 2-acetyloxybenzoic acid (III) with 3-bromophthalide.

1 Los, M.A. (Laboratorios Bagó); Methods of treating mammals suffering from inflammation and pain. BE 0858864; JP 8162049; US 4256760 .
2 Castaner, J.; Prous, J.; Talosalate. Drugs Fut 1986, 11, 5, 394.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(III) 16899 2-(Acetoxy)benzoic acid; Aspirin; Acetylsalicylic acid 50-78-2 C9H8O4 详情 详情
(IV) 24560 3-Bromophthalide; 3-Bromo-2-benzofuran-1(3H)-one 6940-49-4 C8H5BrO2 详情 详情
Extended Information